| Name | 5 HT2C |
|---|---|
| Synonyms | 5 HT 2C; 5 HT2C; 5 HTR2C; 5 hydroxytryptamine (serotonin) receptor 2C; 5 hydroxytryptamine 2C receptor; 5 hydroxytryptamine receptor 2C; 5HT 1C; HTR1C… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 18390444 | Khaliq S, Irfan B, Haider S, Haleem DJ: m-CPP induced hypolocomotion does not interfere in the assessment of memory functions in rats. Pak J Pharm Sci. 2008 Apr;21(2):139-43. Among the multiple classes of receptors described in CNS, much attention has been devoted to the role of 5-HT2C receptor family on memory functions. |
4(0,0,0,4) | Details |
| 12644293 | Nic Dhonnchadha BA, Bourin M, Hascoet M: Anxiolytic-like effects of 5-HT2 ligands on three mouse models of anxiety. Behav Brain Res. 2003 Mar 18;140(1-2):203-14. The behavioural effects of 5-HT (2) receptor agonists, 5-HT (2A) and 5-HT (2C) receptor antagonists were investigated in the mouse four plates test (FPT), light/dark paradigm (L/D) and the elevated plus maze (EPM), in order to elucidate the role of the 5-HT (2) receptor subtypes in these models and to address the inconclusive results previously reported using rat psychopharmacological models. |
4(0,0,0,4) | Details |
| 17240844 | Yamauchi M, Hiraoka S, Imanishi T: [Role of the serotonergic nervous system in anxiety disorders and the anxiolytic mechanism of selective reuptake inhibitors]. Nihon Shinkei Seishin Yakurigaku Zasshi. 2006 Nov;26(5-6):193-8. Previous clinical studies have suggested that the 5-HT2C receptors in subjects with anxiety disorders are hypersensitive. |
2(0,0,0,2) | Details |
| 12646281 | Bull EJ, Hutson PH, Fone KC: Reduced social interaction following 3,4-methylenedioxymethamphetamine is not associated with enhanced 5-HT 2C receptor responsivity. Neuropharmacology. 2003 Mar;44(4):439-48. This study examined the long-term change in serotonergic neuronal function and 5-HT (2C) receptor agonist-induced behaviour following treatment of young rats with 3,4-methylenedioxymethamphetamine (MDMA). |
2(0,0,0,2) | Details |
| 11358463 | Kim D, Murray M, Simansky KJ: The serotonergic 5-HT (2C) agonist m-chlorophenylpiperazine increases weight-supported locomotion without development of tolerance in rats with spinal transections. Exp Neurol. 2001 Jun;169(2):496-500. |
4(0,0,0,4) | Details |
| 18582863 | Kimura Y, Naitou Y, Wanibuchi F, Yamaguchi T: 5-HT (2C) receptor activation is a common mechanism on proerectile effects of apomorphine, and melanotan-II in rats. Eur J Pharmacol. 2008 Jul 28;589(1-3):157-62. Epub 2008 May 24. |
4(0,0,0,4) | Details |
| 12404085 | Jones N, Duxon MS, King SM: 5-HT2C receptor mediation of unconditioned escape behaviour in the unstable elevated exposed plus maze. Psychopharmacology. 2002 Nov;164(2):214-20. Epub 2002 Sep 4. |
4(0,0,0,4) | Details |
| 11564657 | Berg KA, Cropper JD, Niswender CM, Sanders-Bush E, Emeson RB, Clarke WP: RNA-editing of the 5-HT (2C) receptor alters agonist-receptor-effector coupling specificity. Br J Pharmacol. 2001 Sep;134(2):386-92. |
4(0,0,0,4) | Details |
| 12798279 | Graf M, Kantor S, Anheuer ZE, Modos EA, Bagdy G: m-CPP-induced self-grooming is mediated by 5-HT2C receptors. . Behav Brain Res. 2003 Jun 16;142(1-2):175-9. |
4(0,0,0,4) | Details |
| 12690422 | Vickers SP, Easton N, Webster LJ, Wyatt A, Bickerdike MJ, Dourish CT, Kennett GA: Oral administration of the 5-HT2Creceptor agonist, mCPP, reduces body weight gain in rats over 28 days as a result of maintained hypophagia. Psychopharmacology. 2003 May;167(3):274-80. Epub 2003 Apr 11. RATIONALE: The 5-HT (2C) receptor subtype has been implicated extensively in the regulation of ingestive behaviour. |
2(0,0,0,2) | Details |
| 12885442 | Hassanain M, Bhatt S, Siegel A: Differential modulation of feline defensive rage behavior in the medial hypothalamus by 5-HT1A and 5-HT2 receptors. Brain Res. 2003 Aug 15;981(1-2):201-9. The present study was designed to determine the roles played by 5-HT (1A) and 5-HT (2C) receptors in the medial hypothalamus on the expression of defensive rage behavior elicited from electrical stimulation of the PAG. |
2(0,0,0,2) | Details |
| 19058784 | Fujitsuka N, Asakawa A, Hayashi M, Sameshima M, Amitani H, Kojima S, Fujimiya M, Inui A: Selective reuptake inhibitors modify physiological gastrointestinal motor activities via 5-HT2c receptor and acyl ghrelin. Biol Psychiatry. 2009 May 1;65(9):748-59. Epub 2008 Dec 5. |
2(0,0,0,2) | Details |
| 14556235 | Oz M, Zhang L, Rotondo A, Sun H, Morales M: Direct activation by of recombinant human 5-HT1A receptors: comparison with human 5-HT2C and 5-HT3 receptors. Synapse. 2003 Dec 15;50(4):303-13. Magnitudes of maximal DA induced currents were 42 +/- 3% of maximal responses and blocked by the 5-HT2 antagonist, piperazine (1 microM). |
4(0,0,0,4) | Details |
| 11999893 | Schreiber R, De Vry J: Role of 5-hT2C receptors in the hypophagic effect of m-CPP, ORG 37684 and CP-94,253 in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2002 Apr;26(3):441-9. |
4(0,0,0,4) | Details |
| 18256173 | Ward SJ, Lefever TW, Jackson C, Tallarida RJ, Walker EA: Effects of a Cannabinoid1 receptor antagonist and Serotonin2C receptor agonist alone and in combination on motivation for palatable food: a dose-addition analysis study in mice. J Pharmacol Exp Ther. 2008 May;325(2):567-76. Epub 2008 Feb 6. Pretreatment (15 min i.p.) with either the CB (1) receptor antagonist N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-p yrazole-3-carboximide hydrochloride (SR141716) (SR; Rimonabant or Acomplia) or the 5-HT (2C) receptor agonist m-chlorophenylpiperazine (mCPP) dose-dependently decreased the maximum ratio completed under the PR schedule (break point) in mice. |
2(0,0,0,2) | Details |
| 16841562 | Graf M: 5-HT2c receptor activation induces grooming behaviour in rats: possible correlations with obsessive-compulsive disorder. Neuropsychopharmacol Hung. 2006 Mar;8(1):23-8. |
2(0,0,0,2) | Details |
| 19246199 | Kalgutkar AS, Bauman JN, McClure KF, Aubrecht J, Cortina SR, Paralkar J: Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1559-63. Epub 2009 Feb 12. Plausible hypotheses that can collectively account for the differences in mutagenic response of the two piperazine analogs are discussed. |
2(0,0,0,2) | Details |
| 16430857 | Nonogaki K, Ohashi-Nozue K, Oka Y: A negative feedback system between brain systems and plasma active ghrelin levels in mice. Biochem Biophys Res Commun. 2006 Mar 17;341(3):703-7. Epub 2006 Jan 18. Brain systems contribute to regulate eating behavior and energy homeostasis. 5-HT2C receptors and 5-HT1B receptors have been shown to mediate anorexic effects of drugs such as d-fenfluramine, which stimulates release and inhibits reuptake, and m-chlorophenylpiperazine (mCPP), a 5-HT2C receptor agonist. |
2(0,0,0,2) | Details |
| 16914121 | Kao T, Shumsky JS, Jacob-Vadakot S, Himes BT, Murray M, Moxon KA: Role of the 5-HT2C receptor in improving weight-supported stepping in adult rats spinalized as neonates. Brain Res. 2006 Sep 27;1112(1):159-68. Epub 2006 Aug 17. We therefore extended our previous work with the 5-HT2C receptor agonist 1-(m-chlorophenyl)-piperazine hydrochloride (mCPP), which enhances weight-supported stepping when administered to adult rats spinalized as neonates, to identify the optimal dose for improved weight-supported stepping with minimal side effects. |
87(1,1,1,7) | Details |
| 12904965 | Chagraoui A, Protais P, Filloux T, Mocaer E: Agomelatine (S 20098) antagonizes the penile erections induced by the stimulation of 5-HT2C receptors in Wistar rats. Psychopharmacology. 2003 Oct;170(1):17-22. Epub 2003 Aug 7. These compounds were also tested for their ability to inhibit the penile erections induced by the 5-HT (2C) receptor agonists, m-(chlorophenyl) piperazine (mCPP, 0.75 mg/kg, SC) and Ro 60-0175 (2.5 mg/kg, SC) in Wistar rats. |
85(1,1,1,5) | Details |
| 15109520 | Obata H, Saito S, Sakurazawa S, Sasaki M, Usui T, Goto F: Antiallodynic effects of intrathecally administered 5-HT (2C) receptor agonists in rats with nerve injury. Pain. 2004 Mar;108(1-2):163-9. Administration of the 5-HT (2C) receptor agonist, 6-chloro-2-(1-piperazinyl)-pyrazine (MK212; 3-100 microg), 1-(m-chlorophenyl)-piperazine (mCPP; 30-300 microg), or 1-(m-trifluoromethylphenyl)-piperazine (TFMPP; 30-300 microg), produced antiallodynic effects in a dose-dependent manner with no associated motor weakness. |
4(0,0,0,4) | Details |
| 11426831 | Quirk K, Lawrence A, Jones J, Misra A, Harvey V, Lamb H, Revell D, Porter RH, Knight AR: Characterisation of agonist binding on human 5-HT2C receptor isoforms. Eur J Pharmacol. 2001 May 11;419(2-3):107-12. In these studies the affinity of agonists Ro600175 ((S)-2-(6-Chloro-5-fluoroindol-1-yl)-1-methylethylamine), MK212 (6-Chloro-2-(piperazinyl) pyrazine), mCPP (1-(m-chlorophenyl)-piperazine), TfMPP (N-(m-trifluoromethylphenyl) piperazine), DOI (1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane), DOB (1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane) and 8OH-DPAT (8-hydroxy-2-(di-N-propylamino) tetralin) was higher at the INI isoform, whilst antagonist affinity (ketanserin and mesulergine) did not change between the two receptor isoforms. |
4(0,0,0,4) | Details |
| 18439428 | Takeda H, Sadakane C, Hattori T, Katsurada T, Ohkawara T, Nagai K, Asaka M: Rikkunshito, an herbal medicine, suppresses cisplatin-induced anorexia in rats via 5-HT2 receptor antagonism. Gastroenterology. 2008 Jun;134(7):2004-13. Epub 2008 Feb 29. In addition, binding affinities of rikkunshito components were determined in receptor-binding assays using 5-HT2B and 5-HT2C receptors. |
2(0,0,0,2) | Details |
| 17350760 | Bercovici E, Cortez MA, Snead OC 3rd: 5-HT2 modulation of AY-9944 induced atypical absence seizures. . Neurosci Lett. 2007 May 11;418(1):13-7. Epub 2007 Mar 2. We investigated the role of 5-HT (2A) and 5-HT (2C) receptors in atypical absence seizures (AAS) induced by trans-1,4-bis [2-chloro-benzylaminomethyl] cyclohexane, dihydrocholoride (AY-9944). |
2(0,0,0,2) | Details |
| 12734389 | Hajos M, Hoffmann WE, Weaver RJ: Regulation of septo-hippocampal activity by 5-hydroxytryptamine (2C) receptors. J Pharmacol Exp Ther. 2003 Aug;306(2):605-15. Epub 2003 May 6. Intravenous administration of 5-HT2C receptor agonists 1-(3-chlorophenyl) piperazine dihydrochloride (m-CPP) and [S]-2-(chloro-5--indol-1-yl)-1-methyl-ethylamine (Ro 60-0175) dose dependently inhibited firing activity most of the recorded MS/DBv neurons and abolished theta oscillation in all tested MS/DBv and hippocampal neurons. |
84(1,1,1,4) | Details |
| 14699441 | Okada M, Northup JK, Ozaki N, Russell JT, Linnoila M, Goldman D: Modification of human 5-HT (2C) receptor function by Cys23Ser, an abundant, naturally occurring amino-acid substitution. Mol Psychiatry. 2004 Jan;9(1):55-64. |
3(0,0,0,3) | Details |
| 18976545 | Nonogaki K, Ohba Y, Wakameda M, Tamari T: Fluvoxamine exerts anorexic effect in 5-HT2C receptor mutant mice with heterozygous mutation of beta-endorphin gene. Int J Neuropsychopharmacol. 2009 May;12(4):547-52. Epub 2008 Oct 31. |
3(0,0,0,3) | Details |
| 16959056 | Nonogaki K, Nozue K, Takahashi Y, Yamashita N, Hiraoka S, Kumano H, Kuboki T, Oka Y: Fluvoxamine, a selective reuptake inhibitor, and 5-HT2C receptor inactivation induce appetite-suppressing effects in mice via 5-HT1B receptors. Int J Neuropsychopharmacol. 2007 Oct;10(5):675-81. Epub 2006 Sep 7. |
3(0,0,0,3) | Details |
| 15869747 | Voigt JP, Hortnagl H, Rex A, van Hove L, Bader M, Fink H: Brain angiotensin and anxiety-related behavior: the transgenic rat TGR (ASrAOGEN) 680. Brain Res. 2005 Jun 7;1046(1-2):145-56. In the open field, the anxiogenic effect of the 5-HT2C/1B receptor agonist mCPP (0.5-1 mg/kg IP) was more pronounced in TGR (ASrAOGEN) 680. |
1(0,0,0,1) | Details |
| 11041316 | Dekeyne A, Brocco M, Adhumeau A, Gobert A, Millan MJ: The selective (5-HT) 1A receptor ligand, S15535, displays anxiolytic-like effects in the social interaction and Vogel models and suppresses dialysate levels of in the dorsal hippocampus of freely-moving rats. Psychopharmacology. 2000 Sep;152(1):55-66. Its effects were compared with those of other anxiolytic agents: the 5-HT1A agonists, and 8--2-(di-n-propylamino)-tetralin HBr (8-OH-DPAT), the 5-HT2C antagonist, SB206,553 and the benzodiazepine, diazepam. |
1(0,0,0,1) | Details |
| 17935799 | Nunes-de-Souza V, Nunes-de-Souza RL, Rodgers RJ, Canto-de-Souza A: 5-HT2 receptor activation in the midbrain periaqueductal grey (PAG) reduces anxiety-like behaviour in mice. Behav Brain Res. 2008 Feb 11;187(1):72-9. Epub 2007 Aug 30. As mCPP acts preferentially at 5-HT2B and 5-HT2C receptors, Experiment 2 investigated its effects in animals pretreated with ketanserin, a preferential 5-HT2A/2C receptor antagonist. |
1(0,0,0,1) | Details |
| 15733547 | Kommalage M, Hoglund AU: Involvement of spinal serotonin receptors in the regulation of intraspinal release. Eur J Pharmacol. 2005 Feb 21;509(2-3):127-34. Several doses of the receptor agonists 8--2-(di-n-propylamino) tetraline (8-OH-DPAT, 5-HT1A), 1,4-dihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-5H-pyrrolo [3,2-b] pyridin-5- one dihydrochloride (CP93129, 5-HT1B), alpha-methyl- (m5-HT, 5-HT2), 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI, 5-HT2C), and 1-(m-chlorophenyl)-biguanide (5-HT3) were subsequently infused via the microdialysis probe. The 5-HT1A receptor selective antagonist (S)-N-tert-butyl-3-(4-(2-methoxyphenyl) piperazine-1-yl)-2-phenylpropanamid e hydrochloride and the 5-HT2A receptor selective antagonist ketanserin inhibited the 8-OH-DPAT and the m5-HT induced release. |
1(0,0,0,1) | Details |
| 19845681 | Queree P, Peters S, Sharp T: Further pharmacological characterization of 5-HT (2C) receptor agonist-induced inhibition of neuronal activity in the dorsal raphe nucleus in vivo. Br J Pharmacol. 2009 Nov;158(6):1477-85. Epub 2009 Oct 20. The present study extended this pharmacological characterization by comparing the actions of WAY 161503 with the 5-HT (2C) receptor agonists, Ro 60-0275 and 1-(3-chlorophenyl) piperazine (mCPP), as well as the non-selective agonist lysergic acid diethylamide (LSD) and the releasing agent 3,4-methylenedioxymethamphetamine (MDMA). |
84(1,1,1,4) | Details |
| 16165167 | Walker EA, Kohut SJ, Hass RW, Brown EK Jr, Prabandham A, Lefever T: Selective and nonselective antagonists block the aversive stimulus properties of MK212 and m-chlorophenylpiperazine (mCPP) in mice. Neuropharmacology. 2005 Dec;49(8):1210-9. Epub 2005 Sep 13. (2C) (5-HT (2C)) receptors have been implicated to treat mood disorders such as depression and anxiety. |
3(0,0,0,3) | Details |
| 16553644 | Kitazawa T, Ukai H, Komori S, Taneike T: Pharmacological characterization of -induced contraction in the chicken gastrointestinal tract. Auton Autacoid Pharmacol. 2006 Apr;26(2):157-68. The proventriculus (area of stomach adjacent to the oesophagus) and ileum are examined. applied cumulatively caused sustained contraction of the proventriculus that was not decreased by tetrodotoxin, atropine or l-nitro- methylester (l-NAME). alpha-Methyl- showed the same potency as that of indicating the involvement of the 5-HT (2) receptor. (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-amino-propane (DOI), and 1-(3-chlorophenyl) piperazine hydrochloride (mCPP) were potent, and 2-methyl-5-HT, 5-carboxamidotryptamine, BW723C86 and 6-chloro-2-(1-piperazinyl) pyrazine hydrochloride (MK212) were moderate, but (+/-)-8--2-dipropylaminotetralin hydrobromide (8-OH-DPAT), [endo-N-8-methyl-8-azabicyclo-(3,2,1) oct-3-yl]-2,3-dihydro-(1-methyl) ethyl -2-oxo-1H-benzimidazol-1-carboxamide (BIMU-8) and cisapride were weak agonists. Correlation of pEC (50) values of these agonists with documented pEC (50) values for 5-HT (2C) receptor was higher than 5-HT (2A) and 5-HT (2B). |
3(0,0,0,3) | Details |
| 12518270 | Kuhn KU, Quednow BB, Bagli M, Meyer K, Feuchtl A, Westheide J, Frahnert C, Maier W, Rao ML: Allelic variants of the (2C) receptor and neuroendocrinological responses to the (2C) receptor agonist m-chlorophenylpiperazine in healthy male volunteers. Pharmacopsychiatry. 2002 Nov;35(6):226-30. The neurotransmitter possesses several receptors and their subtypes, some of which are polymorphic, such as the 5-HT (2C) receptor. |
3(0,0,0,3) | Details |
| 16307611 | Guitton MJ, Pujol R, Puel JL: m-Chlorophenylpiperazine exacerbates perception of -induced tinnitus in rats. Eur J Neurosci. 2005 Nov;22(10):2675-8. The serotonin receptor 5-HT2c agonist m-chlorophenylpiperazine (mCPP) has been widely used to induce anxiety-like states in animals and anxiety in humans. |
1(0,0,0,1) | Details |
| 15542624 | Lane EL, Cheetham S, Jenner P: uptake inhibitor-induced rotation in -lesioned rats involves both D1 and D2 receptors but is modulated through and receptors. J Pharmacol Exp Ther. 2005 Mar;312(3):1124-31. Epub 2004 Nov 12. The nonspecific ((1/2)) antagonists, methysergide and metergoline, and the specific 5-HT (2C) antagonist, N-desmethylclozapine, enhanced BTS 74 398-induced circling, as did the alpha (2)-adrenoceptor antagonist idazoxan. To determine the involvement of the individual monoamine transporters in the production of motor activity, the effect of the nonselective monoamine uptake inhibitor BTS 74 398 1-([1-(3,4-dichlorophenyl) cyclobutyl]-2-(3-diaminethylaminopropylthio) ethanone monocitrate) and the selective GBR 12909 [1-(2-(bis-(4-fluorphenyl)-methyl) ethyl)-4-(3-phenylpropyl) piperazine) dihydrochloride], (nisoxetine), and (fluvoxamine) reuptake inhibitors on circling in the unilateral -lesioned rat was investigated. |
1(0,0,0,1) | Details |
| 15576070 | Guitton MJ, Dudai Y: Anxiety-like state associates with taste to produce conditioned taste aversion. Biol Psychiatry. 2004 Dec 1;56(11):901-4. METHODS: We have used an anxiogenic agent, the 5-HT2C receptor agonist meta-chlorophenylpiperazine (mCPP), to induce an anxiety-like emotional state in rats after consumption of an unfamiliar tastant. |
1(0,0,0,1) | Details |
| 17936345 | Yonezawa A, Yoshizumi M, Ebiko M, Ise SN, Watanabe C, Mizoguchi H, Kimura Y, Sakurada S: Ejaculatory response induced by a 5-HT2 receptor agonist m-CPP in rats: differential roles of 5-HT2 receptor subtypes. Pharmacol Biochem Behav. 2008 Feb;88(4):367-73. Epub 2007 Sep 18. It has been reported that systemic administration of m-CPP (1-[3-chlorophenyl] piperazine hydrochloride), a 5-HT (2) receptor agonist, produces a 5-HT (2C) receptor-mediated penile erections and self-grooming in rats. |
83(1,1,1,3) | Details |
| 13679227 | Taffe MA, Huitron-Resendiz S, Schroeder R, Parsons LH, Henriksen SJ, Gold LH: MDMA exposure alters cognitive and electrophysiological sensitivity to rapid depletion in rhesus monkeys. Pharmacol Biochem Behav. 2003 Aug;76(1):141-52. Those monkeys were, however, more behaviorally sensitive to challenge with the 5-HT (2C) agonist 1-(3-chlorophenyl) piperazine (mCPP ) 1 year after the MDMA regimen. |
81(1,1,1,1) | Details |
| 15963493 | Matsumoto K, Morishige R, Murakami Y, Tohda M, Takayama H, Sakakibara I, Watanabe H: Suppressive effects of isorhynchophylline on 5-HT2A receptor function in the brain: behavioural and electrophysiological studies. Eur J Pharmacol. 2005 Jul 11;517(3):191-9. Here, we investigated the effects of isorhynchophylline and isorhynchophylline-related alkaloids on receptor-mediated behavioural responses in mice and -evoked current responses in Xenopus oocytes expressing 5-HT2A or 5-HT2C receptors. |
3(0,0,0,3) | Details |
| 12726823 | Mitchell PJ, Fairhall SJ, Fletcher A, Redfern PH: Effects of single and repeated electroconvulsive shock on the social and agonistic behaviour of resident rats. Neuropharmacology. 2003 Jun;44(7):911-25. Additional studies showed that bi-daily ECS treatment nearly abolished 5-HT (2C) receptor-mediated hypolocomotion induced by acute m-chlorophenylpiperazine (mCPP, 2.5 mg/kg sc) challenge 24 h following 2 ECSs, while 4 ECSs only enhanced 5-HT (2A) receptor-mediated head shakes induced by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI, 2.0 mg/kg sc). |
3(0,0,0,3) | Details |
| 18456500 | Yoon J, Yoo EA, Kim JY, Pae AN, Rhim H, Park WK, Kong JY, Park Choo HY: Preparation of piperazine derivatives as 5-HT7 receptor antagonists. . Bioorg Med Chem. 2008 May 15;16(10):5405-12. Epub 2008 Apr 15. Among the synthesized compounds, 3c showed a good activity on 5-HT (7) receptors and a good selectivity on 5-HT (1a), 5-HT (2a), 5-HT (2c), and 5-HT (6) receptors. |
1(0,0,0,1) | Details |
| 14517765 | Sugimoto Y, Inoue K, Yamada J: Involvement of 5-HT (2) receptor in -induced hyperglycemia in mice. Horm Metab Res. 2003 Sep;35(9):511-6. i. p.-induced hyperglycemia was antagonized by the 5-HT (2C/2B) receptor agonist 1-(3-chlorophenyl) piperazine (mCPP), while the 5-HT (2B) receptor agonist BW 723C86 had no effect. These results suggest that -induced hyperglycemia in mice is related to its inhibition of the central 5-HT (2C) receptor. |
1(0,0,0,1) | Details |
| 17451674 | Obata H, Ito N, Sasaki M, Saito S, Goto F: Possible involvement of spinal noradrenergic mechanisms in the antiallodynic effect of intrathecally administered 5-HT2C receptor agonists in the rats with peripheral nerve injury. Eur J Pharmacol. 2007 Jul 12;567(1-2):89-94. Epub 2007 Mar 30. Allodynia was produced by tight ligation of the fifth (L5) and sixth (L6) lumbar spinal nerves on the left side, and was measured by applying von Frey filaments to the left hindpaw. 6-chloro-2-(1-piperazinyl)-pyrazine (MK212; 100 microg) and 1-(m-chlorophenyl)-piperazine (mCPP; 300 microg) were used as 5-HT (2C) receptor agonists. |
36(0,1,1,6) | Details |
| 19066419 | Khan A, Haleem DJ: Responsiveness of 5-HT2C receptors in repeatedly diazepam-injected rats: a behavioral and neurochemical study. Pharmacol Rep. 2008 Sep-Oct;60(5):716-24. The behavioral and neurochemical effects of 1-(m-chlorophenyl) piperazine (m-CPP) (3 mg/kg), a 5-HT2C agonist, were monitored following withdrawal (three days) from two weeks of diazepam administration. |
35(0,1,1,5) | Details |
| 17138863 | Hackler EA, Turner GH, Gresch PJ, Sengupta S, Deutch AY, Avison MJ, Gore JC, Sanders-Bush E: 5-Hydroxytryptamine2C receptor contribution to m-chlorophenylpiperazine and N-methyl-beta-carboline-3-carboxamide-induced anxiety-like behavior and limbic brain activation. J Pharmacol Exp Ther. 2007 Mar;320(3):1023-9. Epub 2006 Nov 30. Activation of 5-hydroxytryptamine2C (5-HT (2C)) receptors by the 5-HT (2) receptor agonist m-chlorophenylpiperazine (m-CPP) elicits anxiety in humans and anxiety-like behavior in animals. |
3(0,0,0,3) | Details |
| 11888560 | Hewitt KN, Lee MD, Dourish CT, Clifton PG: 2C receptor agonists and the behavioural satiety sequence in mice. Pharmacol Biochem Behav. 2002 Apr;71(4):691-700. Behavioural satiety sequence (BSS) and food intake measurements were taken, comparing the selective 5-HT (2C) receptor agonist (S)-2-(6-chloro-5--indol-l-yl)-l-methylethylamine hydrochloride (Ro 60-0175; 1.0, 3.0 and 10.0 mg/kg) and D-fenfluramine (3.0 mg/kg). The 5-HT (1B/2C) receptor agonist 1-(m-chlorophenyl) piperazine (mCPP; 3 mg/kg) also produced a substantial decrease in food intake, which was attenuated by SB 242084 (0.5 mg/kg). |
3(0,0,0,3) | Details |
| 15075625 | Alves SH, Pinheiro G, Motta V, Landeira-Fernandez J, Cruz AP: Anxiogenic effects in the rat elevated plus-maze of 5-HT (2C) agonists into ventral but not dorsal hippocampus. Behav Pharmacol. 2004 Feb;15(1):37-43. The effect of the non-selective 5-HT2C receptor agonist trifluoromethyl-phenylpiperazine (TFMPP, 0.75, 1.5 and 3.0 microg) and the preferential 5-HT2C agonist 6-chloro-2 (1-piperazinyl) pyrazine (MK-212, 0.1, 0.3 and 1.0 microg) microinjected into the ventral or dorsal hippocampus was investigated in anxiety measures of rats exposed to the elevated plus-maze test. |
1(0,0,0,1) | Details |
| 17942093 | Wang R, Xu Y, Wu HL, Li YB, Li YH, Guo JB, Li XJ: The antidepressant effects of in the forced swimming test involve 5-HT1 and 5-HT2 receptors. Eur J Pharmacol. 2008 Jan 6;578(1):43-50. Epub 2007 Sep 19. Taken together, these results indicate that the antidepressant-like effect of in the forced swimming test is related to serotonergic system and may be mediated by, at least in part, an interaction with 5-HT (1A/1B) and 5-HT (2C) receptors. |
1(0,0,0,1) | Details |
| 15582454 | Chu W, Tu Z, McElveen E, Xu J, Taylor M, Luedtke RR, Mach RH: Synthesis and in vitro binding of N-phenyl piperazine analogs as potential D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87. Binding studies were also conducted to determine if the compounds bound to sigma (sigma (1) and sigma (2)) and (5-HT (1A), 5-HT (2A), 5-HT (2B), 5-HT (2C), 5-HT (3), 5-HT (4), 5-HT (5), 5-HT (6), and 5-HT (7)) receptors. |
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| 15896731 | Mosher T, Hayes D, Greenshaw A: Differential effects of 5-HT2C receptor ligands on place conditioning and locomotor activity in rats. Eur J Pharmacol. 2005 May 16;515(1-3):107-16. Effects of the (5-HT)(1A/1B/2C) receptor agonist N-[3-(trifluoromethyl) phenyl] piperazine (TFMPP, 0-3.0 mg/kg s.c.) and the 5-HT2C receptor agonist 8,9-dichloro-2,3,4,4a-tetrahydro-1H-pyrazino [1,2-a] quinoxalin-5 (6H)-one (WAY 161503, 0-3.0 mg/kg s.c.) in place conditioning were measured in male Sprague-Dawley rats. |
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| 15113845 | Schlag BD, Lou Z, Fennell M, Dunlop J: Ligand dependency of 5-hydroxytryptamine 2C receptor internalization. J Pharmacol Exp Ther. 2004 Sep;310(3):865-70. Epub 2004 Apr 27. In this study, we have examined the effects of 5-HT2C receptor agonists Ro 60-0175 [(S)-2-(6-chloro-5-fluoroindol-1-yl)-1-methylethylamine], and WAY-161503 [(4aR)-8,9-dichloro-2,3,4,4a-tetrahydro-1H-pyrazino [1,2-a] quinoxalin-5 (6H) -one]; partial agonists mCPP [1-(m-chlorophenyl) piperazine] and DOI [(+)-1-(2,5-dimethoxy-4-iodophenyl)-2-amino-propane]; inverse agonists SB-206553 [N-3-pyridinyl-3,5-dihydro-5-methylbenzo (1,2-b:4,5-b') dipyrrole-1 (2H) carbo xamide] and mianserin; and neutral antagonists SB-242084 [6-chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl) oxy]-5-pyridyl] carbamoyl]-in doline] and 5-methoxygramine on the internalization of a C-terminal green fluorescent protein (GFP)-tagged 5-HT2C receptor (VSV isoform) expressed in transiently transfected human embryonic kidney cells. |
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| 15107597 | Kovacs A, Gacsalyi I, Wellmann J, Schmidt E, Szucs Z, Dubreuil V, Nicolas JP, Boutin J, Bozsing D, Egyed A, Tihanyi K, Spedding M, Szenasi G: Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther. 2003 Sep-Nov;17(5-6):427-34. Our aim was to specify the 5-HT (2) subtype selectivity of EGIS-7625 (1-benzyl-4-[(2-nitro-4-methyl-5-amino)-phenyl]-piperazine), a new 5-HT (2B) ligand, in receptor binding studies and characterize its pharmacology at 5-HT (2A), 5-HT (2B) and 5-HT (2C) receptors in in vivo experiments and in isolated organs, in vitro. |
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| 18614422 | Samad N, Haleem MA, Haleem DJ: Behavioral effects of 1-(m-chlorophenyl) piperazine (m-CPP) in a rat model of tardive dyskinesia. Pak J Pharm Sci. 2008 Jul;21(3):262-8. The behavioral effects of 1-(m-chlorophenyl) piperazine (m-CPP) a 5-HT-2C and 5-HT-1B agonist were monitored 2 days after 5 weeks of saline or haloperidol administration. |
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| 11267640 | Mehta A, Eberle-Wang K, Chesselet MF: Increased m-CPP-induced oral dyskinesia after lesion of serotonergic neurons. Pharmacol Biochem Behav. 2001 Feb;68(2):347-53. Peripheral administration of the (5-HT)(2C/1B) agonist 1-(m-chlorophenyl) piperazine (m-CPP) produces abnormal orofacial movements in rats. We have previously shown that this behavior is mediated by 5-HT (2C) receptors in the subthalamic nucleus [Neuroscience 72 (1996) 117]. |
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| 11856898 | Gleason SD, Lucaites VL, Shannon HE, Nelson DL, Leander JD: m-CPP hypolocomotion is selectively antagonized by compounds with high affinity for 5-HT (2C) receptors but not 5-HT (2A) or 5-HT (2B) receptors. Behav Pharmacol. 2001 Dec;12(8):613-20. The ability of m-CPP [1-(m-chlorophenyl) piperazine] to produce hypolocomotion is well documented. This effect has been postulated to be due to activation of the 5-HT (2C) receptor. |
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| 19523439 | Nonogaki K, Kaji T, Ohba Y, Sumii M, Wakameda M, Tamari T: 5-HT2C receptor-independent expression of hypothalamic NOR1, a novel modulator of food intake and energy balance, in mice. Biochem Biophys Res Commun. 2009 Aug 21;386(2):311-5. Epub 2009 Jun 10. These findings suggest that 5-HT2C receptor-independent proopiomelanocortin-derived peptides regulate the expression of hypothalamic NOR1, which is a novel modulator of feeding behavior and energy balance. |
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| 19875674 | Rasbach KA, Funk JA, Jayavelu T, Green PT, Schnellmann RG: 5-hydroxytryptamine receptor stimulation of mitochondrial biogenesis. J Pharmacol Exp Ther. 2010 Feb;332(2):632-9. Epub 2009 Oct 29. Reverse transcription-polymerase chain reaction analysis confirmed the presence of 5-HT2A, 5-HT2B, and 5-HT2C receptor mRNA in RPTC. |
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| 15638778 | Isaac M: Serotonergic 5-HT2C receptors as a potential therapeutic target for the design antiepileptic drugs. Curr Top Med Chem. 2005;5(1):59-67. More specifically, the recent finding that the 5-HT2B/2C receptor agonist, 1-(m-chlorophenyl)-piperazine (mCPP) is anticonvulsant has kindled an interest into the investigation of the serotonergic 5-HT2C receptor subtype as a potential target for the treatment of epilepsy. |
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| 12218511 | Miranda F, Orozco G, Velazquez-Martinez DN: Full substitution of the discriminative cue of a 5-HT (1A/1B/2C) agonist with the combined administration of a 5-HT (1B/2C) and a 5-HT (1A) agonist. Behav Pharmacol. 2002 Jul;13(4):303-11. In generalization tests, INDO, 8--2-(di-n-propylamino) tetralin (8-OH-DPAT, a 5-HT (1A) agonist), 1-(3-trifluoromethylphenyl) piperazine (TFMPP, a 5-HT (1B) agonist), alpha-methyl- (a 5-HT (2C) agonist) or 2-methyl- (a 5-HT (3) agonist), were administered alone or in combination. |
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| 17059817 | Monti JM, Jantos H: Effects of the 5-HT2A/2C receptor agonist DOI and of the selective 5-HT2A or 5-HT2C receptor antagonists EMD 281014 and SB-243213, respectively, on sleep and waking in the rat. Eur J Pharmacol. 2006 Dec 28;553(1-3):163-70. Epub 2006 Sep 23. The effects of the 5-HT (2A/2C) receptor agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and of the selective 5-HT (2A) or 5-HT (2C) receptor antagonists 7-{4-[2-(4--phenyl)-ethyl]-piperazine-1-carbonyl}-1H--3-carbon itrile HCl (EMD 281014) and 5-methyl-1-[[-2-[(2-methyl-3-pyridyl) oxy]-5-pyridyl] carbamoyl]-6-trifluoro methylindoline HCl (SB-243213), respectively, on spontaneous sleep were studied in adult rats implanted for chronic sleep recordings. |
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| 19402569 | Samad N, Haleem DJ: Behavioral and neurochemical profile of m-CPP following exposure to single restraint stress in rat. Acta Neurol Belg. 2009 Mar;109(1):24-31. Rats were restrained for 2 hours. 24-h after the termination of the restraint period, 1-(m-Chlorophenyl) piperazine (m-CPP; a 5-HT-2C agonist) at the doses of 1.5 mg/kg or 3.0 mg/kg and saline (1 ml/kg), was injected to unrestrained and restrained animals. |
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| 11101359 | Ravina E, Casariego I, Masaguer CF, Fontenla JA, Montenegro GY, Rivas ME, Loza MI, Enguix MJ, Villazon M, Cadavid MI, Demontis GC: Conformationally constrained butyrophenones with affinity for (D (1), D (2), D (4)) and (5-HT (2A), 5-HT (2B), 5-HT (2C)) receptors: synthesis of aminomethylbenzo [b] furanones and their evaluation as antipsychotics. J Med Chem. 2000 Nov 30;43(24):4678-93. A series of novel conformationally restricted butyrophenones (6-aminomethyl-4,5,6,7-tetrahydrobenzo [b] furan-4-ones bearing 4-(6-fluorobenzisoxazolyl) piperidine, 4-(p-fluorobenzoyl) piperidine, 4-(o-methoxyphenyl) piperazine, 4-(2-pyridyl) piperazine, 4-(2-pyrimidinyl) piperazine, or linear butyro (or valero) phenone fragments) were prepared and evaluated as antipsychotic agents by in vitro assays for affinity for receptors (D (1), D (2), D (4)) and serotonin receptors (5-HT (2A), 5-HT (2B), 5-HT (2C)), by neurochemical studies, and by in vivo assays for antipsychotic potential and the risk of inducing extrapyramidal side effects. |
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| 11011047 | Yamada J, Sugimoto Y: The 5-HT (2C/2B) receptor agonist, m-chlorophenylpiperazine, increases plasma glucagon levels in rats. Eur J Pharmacol. 2000 Oct 6;406(1):153-7. |
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| 11509227 | Vickers SP, Easton N, Malcolm CS, Allen NH, Porter RH, Bickerdike MJ, Kennett GA: Modulation of 5-HT (2A) receptor-mediated head-twitch behaviour in the rat by 5-HT (2C) receptor agonists. Pharmacol Biochem Behav. 2001 Jul-Aug;69(3-4):643-52. The preferential 5-HT (2C) receptor agonists Ro 60-0175, 6-chloro-2-[1-piperazinyl]-pyrazine HCl (MK-212), 1-(3-chlorophenyl) piperazine hydrochloride (mCPP), 1-(3-trifluoromethylphenyl) piperazine hydrochloride (TFMPP), and (S)-3-[(2,3-dihydro-5-methoxy-1H-inden-4-yl) oxy]-pyrollidine HCl (ORG-37684), the 5-HT (2A/2C) receptor agonist 2,5-dimethoxy-4-iodoamphetamine (DOI), the 5-HT (2B) receptor agonist 1-[5-thienylmethoxy-1-1H-3-indoyl] propan-2-amine hydrochloride (BW-723C86), and nor-D-fenfluramine were administered to rats subsequent to an acute challenge of SB-242084. |
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| 19133244 | Zhang QJ, Liu X, Liu J, Wang S, Ali U, Wu ZH, Wang T: Subthalamic neurons show increased firing to 5-HT2C receptor activation in -lesioned rats. Brain Res. 2009 Feb 23;1256:180-9. Epub 2008 Dec 24. |
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| 12534984 | Clifton PG, Lee MD, Somerville EM, Kennett GA, Dourish CT: 5-HT1B receptor knockout mice show a compensatory reduction in 5-HT2C receptor function. Eur J Neurosci. 2003 Jan;17(1):185-90. |
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| 15118345 | Calama E, Moran A, Ortiz de Urbina AV, Martin ML, San Roman L: Vasoconstrictor responses to in the autoperfused hindquarters of spontaneously hypertensive rats. Pharmacology. 2004 Jun;71(2):66-72. Our data suggest that the vasoconstrictor response induced by in the autoperfused hindquarters of SHR is mainly mediated by the activation of 5-HT2A and 5-HT2C receptors. |
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| 12892833 | Zanoveli JM, Nogueira RL, Zangrossi H Jr: in the dorsal periaqueductal gray modulates inhibitory avoidance and one-way escape behaviors in the elevated T-maze. Eur J Pharmacol. 2003 Jul 25;473(2-3):153-61. Taken altogether, our findings suggest that 5-HT1A and 5-HT2c receptors in the dorsal periaqueductal gray exert opposed control on inhibitory avoidance, implicating these receptors in anxiety conditioning. |
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| 12202639 | Mori A, Kogo M, Ishihama K, Tanaka S, Enomoto A, Koizumi H, Matsuya T: Effect of on trigeminal rhythmic activities generated in in vitro brainstem block preparations. J Dent Res. 2002 Sep;81(9):598-602. In the present study, both the 5-HT (1A) phthalimido-butyl-piperazine, and the 5-HT (2C) agonist, 1-2,5-dimethoxy-4-iodophenyl-2-aminopropane, combined with N-methyl-D,L- and bicuculline, elicited trigeminal rhythmic activities in a whole brainstem block preparation. |
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| 16470405 | Dalton GL, Lee MD, Kennett GA, Dourish CT, Clifton PG: 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse. Psychopharmacology. 2006 Mar;185(1):45-57. Epub 2006 Feb 10. RATIONALE: To examine the functional relationship between 5-HT1B receptors (5-HT1B-R) and 5-HT2C receptors (5-HT2C-R) in the control of food intake. |
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| 11763004 | Scheepers FE, Gespen de Wied CC, Kahn RS: The effect of treatment on m-chlorophenylpiperazine-induced hormone release in schizophrenia. J Clin Psychopharmacol. 2001 Dec;21(6):575-82. The present study investigated whether treatment with blocks hormone release induced by the 5-HT2c agonist m-chlorophenylpiperazine (m-CPP) and, if so, whether this antagonistic effect is related to treatment response. |
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| 19420729 | Yonezawa A, Yoshizumi M, Ise SN, Watanabe C, Mizoguchi H, Furukawa K, Tsuru H, Kimura Y, Kawatani M, Sakurada S: Synergistic actions of apomorphine and m-chlorophenylpiperazine on ejaculation, but not penile erection in rats. Biomed Res. 2009 Apr;30(2):71-8. It has been suggested that (DA) and and their receptors, particularly D (2)-like and 5-HT (2C) receptors, may play a significant role in the control of male sexual function. |
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| 18644367 | Moran A, Ortiz de Urbina AV, Martin ML, Garcia M, Rodriguez-Barbero A, Dorado F, San Roman L: Characterization of contractile 5-hydroxytryptamine receptor subtypes in the in situ autoperfused kidney in the anaesthetized rat. Eur J Pharmacol. 2008 Sep 11;592(1-3):133-7. Epub 2008 Jul 4. The selective 5-HT2 receptor agonist alpha-methyl- (alpha-methyl- and the non-selective 5-HT2C receptor agonist (1-(3-chlorophenyl) piperazine), m-CPP, caused a local vasoconstrictor effect in the autoperfused rat kidney, whereas BW723C86, a selective 5-HT2B receptor agonist, the 5-HT1 receptor agonist 5-carboxamidotryptamine, 5-CT, and the selective 5-HT3 receptor agonist m-CPBG (1-(m-chlorophenyl)-biguanide) did not modify the renal perfusion pressure. The results of protein expression analyses allow us to postulate that 5HT-SRC (a 5-HT2C receptor protein) is expressed in renal tissue and differentially expressed in renal artery. |
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| 11906967 | Centurion D, Ortiz MI, Saxena PR, Villalon CM: The atypical 5-HT2 receptor mediating tachycardia in pithed rats: pharmacological correlation with the 5-HT2A receptor subtype. Br J Pharmacol. 2002 Mar;135(6):1531-9. Since 5-HT (2) receptors consist of 5-HT (2A), 5-HT (2B) and 5-HT (2C) subtypes, this study investigated if these subtypes mediate the above response. 2. In pithed rats, intraperitoneally (i.p.) pre-treated with reserpine (5 mg kg (-1)), intravenous (i.v.) administration of 5-HT, 5- (5-MeO-T), 1-(3-chlorophenyl) piperazine (mCPP) and 5-carboxamidotryptamine (5-CT) (10, 30, 100 and 300 microg kg (-1) each), produced dose-dependent tachycardic responses. |
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| 12625876 | Zhelyazkova-Savova MD, Zhelyazkov DK: Behavioural evidence of agonist-like effect of isoteoline at 5-HT1B serotonergic receptors in mice. J Pharm Pharmacol. 2003 Jan;55(1):125-9. Previous studies with isoteoline have shown antagonistic activity at 5-HT (2C) serotonergic receptors. In our study, we used N-(3-trifluoromethylphenyl) piperazine (TFMPP) (2 mg kg (-1)) as a reference agonist at these receptor sites. |
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| 15619112 | Bert B, Felicio LF, Fink H, Nasello AG: The use of sudden darkness in mice: a behavioural and pharmacological approach. Psychopharmacology. 2005 Jun;179(4):846-53. Epub 2004 Dec 24. In the second part, responses to the 5-HT (1A) receptor agonist 8-OH-DPAT (0.5 and 1.0 mg/kg) and 5-HT (2C) receptor agonist mCPP (1.0 and 2.0 mg/kg) were investigated in male Swiss mice. |
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| 17207863 | Cornelio AM, Nunes-de-Souza RL: Anxiogenic-like effects of mCPP microinfusions into the amygdala (but not dorsal or ventral hippocampus) in mice exposed to elevated plus-maze. Behav Brain Res. 2007 Mar 12;178(1):82-9. Epub 2007 Jan 17. This anxiogenic-like effect of mCPP was selectively and completely blocked by local injection of a behaviourally-inactive dose of SDZ SER-082 (10nmol/0.1microl), a preferential 5-HT (2C) receptor antagonist. |
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| 14996544 | Dalton GL, Lee MD, Kennett GA, Dourish CT, Clifton PG: mCPP-induced hyperactivity in 5-HT2C receptor mutant mice is mediated by activation of multiple receptor subtypes. Neuropharmacology. 2004 Apr;46(5):663-71. |
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| 11082448 | Cryan JF, Lucki I: Antidepressant-like behavioral effects mediated by 5-Hydroxytryptamine (2C) receptors. J Pharmacol Exp Ther. 2000 Dec;295(3):1120-6. |
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| 19501602 | Fletcher PJ, Tampakeras M, Sinyard J, Slassi A, Isaac M, Higgins GA: Characterizing the effects of 5-HT (2C) receptor ligands on motor activity and feeding behaviour in 5-HT (2C) receptor knockout mice. Neuropharmacology. 2009 Sep;57(3):259-67. Epub 2009 Jun 6. |
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| 15804427 | Ferreira HS, Oliveira E, Faustino TN, Silva Ede C, Fregoneze JB: Effect of the activation of central 5-HT2C receptors by the 5-HT2C agonist mCPP on blood pressure and heart rate in rats. Brain Res. 2005 Apr 8;1040(1-2):64-72. |
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| 12151028 | Rice HB, Corwin RL: mCPP-induced hypophagia in rats is unaffected by the profile of dietary unsaturated fatty acids. Pharmacol Biochem Behav. 2002 Oct;73(3):545-50. Evidence suggests an association between the 5-HT (2C) receptor and fat intake. The effects of 1-(3-chlorophenyl) piperazine (mCPP) on consumption of both low-fat (Experiment 1) and high-fat diets (Experiment 2) differing in their predominant PUFA profiles were compared in rats. |
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| 11063789 | Terao T, Nakamura J, Yoshimura R, Ohmori O, Takahashi N, Kojima H, Soeda S, Shinkai T, Nakano H, Okuno T: Relationship between serum levels and meta-chlorophenylpiperazine-induced responses in healthy men and women. Psychiatry Res. 2000 Oct 30;96(2):167-73. In the human brain, m-CPP binds both to various serotonergic receptors, mainly 5-HT (2C), and to alpha (2)-adrenoceptors. |
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| 11432685 | Broocks A, Meyer T, Gleiter CH, Hillmer-Vogel U, George A, Bartmann U, Bandelow B: Effect of aerobic exercise on behavioral and neuroendocrine responses to meta-chlorophenylpiperazine and to ipsapirone in untrained healthy subjects. Psychopharmacology. 2001 May;155(3):234-41. CONCLUSIONS: Regular aerobic exercise is associated with a blunted response to m-CPP, which might reflect a downregulation of central 5-HT2C receptors. |
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| 16549369 | Stark JA, Davies KE, Williams SR, Luckman SM: Functional magnetic resonance imaging and c-Fos mapping in rats following an anorectic dose of m-chlorophenylpiperazine. Neuroimage. 2006 Jul 1;31(3):1228-37. Epub 2006 Mar 20. Activity in the limbic system may reflect the appetitive agonist activity of mCPP at the 5-HT (2C) receptor. |
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| 12850497 | Gatch MB: Discriminative stimulus effects of m-chlorophenylpiperazine as a model of the role of serotonin receptors in anxiety. Life Sci. 2003 Aug 1;73(11):1347-67. The roles of reuptake and 5-HT1A receptors have been well characterized, but the contribution of other serotonin receptor subtypes is not as clear. 1-(3-Chlorophenyl)-piperazine (mCPP), which binds non-selectively to a wide range of serotonin receptors, has often been used to produce anxiety in humans and in animal models. Because functional assays indicate that mCPP is significantly more potent at 5-HT2C receptors, it may serve as a tool to investigate the contribution of 5-HT2C receptors to anxiety. |
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| 11205420 | Duxon MS, Stretton J, Starr K, Jones DN, Holland V, Riley G, Jerman J, Brough S, Smart D, Johns A, Chan W, Porter RA, Upton N: Evidence that orexin-A-evoked grooming in the rat is mediated by orexin-1 (OX1) receptors, with downstream 5-HT2C receptor involvement. Psychopharmacology. 2001 Jan 1;153(2):203-9. |
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| 11311410 | Takahashi H, Takada Y, Urano T, Takada A: Dissociation of systemic and hippocampal modulation of rat locomotor activity by 5-HT (2C) receptors. Neurosci Res. 2001 May;40(1):97-103. |
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| 15551195 | Kuhn KU, Joe AY, Meyer K, Reichmann K, Maier W, Rao ML, Reinhardt MJ, Biersack HJ, Quednow BB: Neuroimaging and 5-HT2C receptor polymorphism: a HMPAO-SPECT study in healthy male probands using mCPP-challenge of the 5-HT2C receptor. Pharmacopsychiatry. 2004 Nov;37(6):286-91. |
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| 15234597 | Simansky KJ, Dave KD, Inemer BR, Nicklous DM, Padron JM, Aloyo VJ, Romano AG: A 5-HT2C agonist elicits hyperactivity and oral dyskinesia with hypophagia in rabbits. Physiol Behav. 2004 Aug;82(1):97-107. |
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| 12467943 | Klaassen T, Riedel WJ, van Praag HM, Menheere PP, Griez E: Neuroendocrine response to meta-chlorophenylpiperazine and ipsapirone in relation to anxiety and aggression. Psychiatry Res. 2002 Dec 15;113(1-2):29-40. Fifteen patients and 16 normal controls received single oral doses of 0.5 mg/kg meta-chlorophenylpiperazine (MCPP), a 5-HT (2C) agonist, and 10 mg of ipsapirone, a 5-HT (1A) agonist, according to a double-blind, placebo-controlled, cross-over design. |
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| 15866558 | Tsaltas E, Kontis D, Chrysikakou S, Giannou H, Biba A, Pallidi S, Christodoulou A, Maillis A, Rabavilas A: Reinforced spatial alternation as an animal model of obsessive-compulsive disorder (OCD): investigation of 5-HT2C and 5-HT1D receptor involvement in OCD pathophysiology. Biol Psychiatry. 2005 May 15;57(10):1176-85. |
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| 14979792 | Frankel PS, Cunningham KA: m-Chlorophenylpiperazine (mCPP) modulates the discriminative stimulus effects of cocaine through actions at the 5-HT2C receptor. Behav Neurosci. 2004 Feb;118(1):157-62. |
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| 17344339 | Kalgutkar AS, Dalvie DK, Aubrecht J, Smith EB, Coffing SL, Cheung JR, Vage C, Lame ME, Chiang P, McClure KF, Maurer TS, Coelho RV Jr, Soliman VF, Schildknegt K: Genotoxicity of 2-(3-chlorobenzyloxy)-6-(piperazinyl) pyrazine, a novel 5-hydroxytryptamine2c receptor agonist for the treatment of obesity: role of metabolic activation. Drug Metab Dispos. 2007 Jun;35(6):848-58. Epub 2007 Mar 7. 2-(3-Chlorobenzyloxy)-6-(piperazin-1-yl) pyrazine (3) is a potent and selective 5-HT (2C) agonist that exhibits dose-dependent inhibition of food intake and reduction in body weight in rats, making it an attractive candidate for treatment of obesity. The mass spectrum of the amine conjugate was consistent with condensation of amine with an metabolite derived from hydroxylation of the secondary piperazine -alpha-carbon bond. |
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| 11352361 | Vassallo CM, Feldman E, Peto T, Castell L, Sharpley AL, Cowen PJ: Decreased availability but normal post-synaptic 5-HT2c receptor sensitivity in chronic fatigue syndrome. Psychol Med. 2001 May;31(4):585-91. |
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| 11888572 | Fone KC, Topham IA: Alteration in agonist-induced behaviour following a implant in adult rats. Pharmacol Biochem Behav. 2002 Apr;71(4):815-23. The elevation in plasma and back muscle contractions evoked by the 5-HT (2A) agonist DOI (1 mg/kg ip) were attenuated, whilst wet-dog shakes were enhanced by treatment. 5-HT (2B) agonist-induced behaviour and the hypolocomotion and hypophagia induced by the 5-HT (2C) agonist m-CPP (2.5 mg/kg ip) were unaltered but the mCPP-induced elevation in was abolished by treatment. |
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| 11198050 | Wilson AW, Costall B, Neill JC: Manipulation of operant responding for an -paired conditioned stimulus in the rat by pharmacological alteration of the serotonergic system. J Psychopharmacol. 2000;14(4):340-6. Results showed that the releaser d-fenfluramine, the selective reuptake inhibitor fluoxetine, the 5-HT1A receptor agonist 8--2 [di-n-propylamino] tetralin, the partial 5-HT1A receptor agonist and the 5-HT1B/5-HT2C receptor agonist 1-(3-trifluoromethylphenyl) piperazine, but not the 5-HT2A/5-HT2C receptor agonist 1-(2,5-dimethoxy-4-iodophenylaminopropane)-2, selectively reduced responding on a lever leading to presentation of an paired conditioned stimulus. |
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| 20347301 | Fiorino F, Severino B, De Angelis F, Perissutti E, Magli E, Frecentese F, Esposito A, Massarelli P, Nencini C, Santagada V, Caliendo G: New 5-HT (1A) receptor ligands containing a N'-cyanoisonicotinamidine nucleus: Synthesis and in vitro pharmacological evaluation. Bioorg Med Chem Lett. 2010 Mar 3. The combination of structural elements (heterocyclic nucleus, alkyl chain and 4-substituted piperazine) known to be critical in order to have affinity on 5-HT (1A) receptor and the proper selection of substituents led to compounds with high specificity and affinity towards serotoninergic receptors. |
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| 16049570 | El Mansari M, Blier P: Responsiveness of 5-HT (1A) and 5-HT2 receptors in the rat orbitofrontal cortex after long-term reuptake inhibition. J Psychiatry Neurosci. 2005 Jul;30(4):268-74. RESULTS: After administration of paroxetine for either 3 weeks or 8 weeks, there was no modification in the inhibitory effect of the preferential 5-HT (2A) receptor agonist (+)-1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane hydrochloride (DOI) or the preferential 5-HT (2C) receptor agonist 3-chlorophenyl piperazine dihydrochloride (mCPP). |
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| 16173953 | Calama E, Ortiz de Urbina AV, Moran A, Martin ML, San Roman L: Effect of on neurogenic vasoconstriction in the isolated, autoperfused hindquarters of the rat. Clin Exp Pharmacol Physiol. 2005 Oct;32(10):894-900. The effects of were mimicked by 5-carboxamidotryptamine (a 5-HT1 receptor agonist) and L-694 247 (a selective 5-HT1D receptor agonist), but not by 8--2-dipropylaminotetralin (a 5-HT1A receptor agonist), CGS-12066B (a 5-HT1B receptor agonist), alpha-methyl- (a 5-HT2 receptor agonist), 1-(3-chlorophenyl) piperazine (a 5-HT2C receptor agonist) or 1-phenylbiguanide (a 5-HT3 receptor agonist). |
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| 19699736 | Moran A, de Urbina AV, Martin ML, Rodriguez-Barbero A, Roman LS: Characterization of the contractile 5-hydroxytryptamine receptor in the autoperfused kidney of L-NAME hypertensive rats. Eur J Pharmacol. 2009 Oct 12;620(1-3):90-6. Epub 2009 Aug 21. The selective 5-HT (2B) receptor agonist BW723C86, the non-selective 5-HT (2C) receptor agonist (1-(3-chlorophenyl) piperazine), m-CPP, the (1) receptor agonist 5-carboxamidotryptamine (5-CT) and the selective 5-HT (3) receptor agonist (1-(m-chlorophenyl)-biguanide), m-CPBG, did not modify renal perfusion pressure. |
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| 16242827 | Antonatos S, Galanopoulou P: Effects of mu-CPP and mesulergine on dietary choices in deprived rats: possible mechanisms of their action. Prog Neuropsychopharmacol Biol Psychiatry. 2006 Jan;30(1):112-9. Epub 2005 Oct 20. Although it has been well established that compounds that stimulate 5-HT (2C) and/or 5-HT (1B) receptors induce hypophagia by promoting satiety process, the relative role of these receptor subtypes in dietary choices remains to be fully determined. m-CPP is considered a useful probe of 5-HT (2C) receptor function in vivo and its administration reduces food intake and appetite in humans and rats. |
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| 15301922 | Yamauchi M, Tatebayashi T, Nagase K, Kojima M, Imanishi T: Chronic treatment with fluvoxamine desensitizes 5-HT2C receptor-mediated hypolocomotion in rats. Pharmacol Biochem Behav. 2004 Aug;78(4):683-9. |
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| 16973729 | Nonogaki K, Nozue K, Oka Y: Hyperphagia alters expression of hypothalamic 5-HT2C and 5-HT1B receptor genes and plasma des-acyl ghrelin levels in Ay mice. Endocrinology. 2006 Dec;147(12):5893-900. Epub 2006 Sep 14. |
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| 11806866 | Bagdy G, Graf M, Anheuer ZE, Modos EA, Kantor S: Anxiety-like effects induced by acute fluoxetine, or m-CPP treatment are reversed by pretreatment with the 5-HT2C receptor antagonist SB-242084 but not the 5-HT1A receptor antagonist WAY-100635. Int J Neuropsychopharmacol. 2001 Dec;4(4):399-408. The possible role of 5-HT1A and 5-HT2C receptors in the anxiety induced by fear, acute treatment with SSRI antidepressants or the receptor agonist m-CPP were tested in the social interaction anxiety test in male Sprague-Dawley rats. |
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| 17983585 | Zhou L, Sutton GM, Rochford JJ, Semple RK, Lam DD, Oksanen LJ, Thornton-Jones ZD, Clifton PG, Yueh CY, Evans ML, McCrimmon RJ, Elmquist JK, Butler AA, Heisler LK: 2C receptor agonists improve type 2 diabetes via melanocortin-4 receptor signaling pathways. Cell Metab. 2007 Nov;6(5):398-405. We report here that 2C receptor (5-HT (2C) R) agonists, typically investigated for their anorectic properties, significantly improve tolerance and reduce plasma insulin in murine models of obesity and type 2 diabetes. |
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| 15452415 | Calama E, Moran A, Ortiz de Urbina AV, Martin ML, San Roman L: m-CPP, a 5-HT2C receptor agonist that modifies the perfusion pressure of the hindquarter vascular bed of anesthetized rat. Pharmacology. 2005 Feb;73(2):70-5. Epub 2004 Sep 27. Both vasodilatation and vasoconstriction were inhibited by the (1,2 ) receptor antagonist methiothepin, whereas the 5-HT (2 ) receptor antagonist ritanserin blocked only the vasoconstrictor responses. 1-[4-(1-Adamantanecarboxamido) butyl]-4-(2-methoxyphenyl) piperazine (a 5-HT (1A) receptor antagonist) and ICI 118,551 (a beta (2)-receptor antagonist) failed to modify the vasodilator responses of m-CPP. |
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| 11767117 | Sugimoto Y, Yoshikawa T, Noma T, Yamada J: The 5-HT2C/2B receptor agonist m-chlorophenylpiperazine (mCPP) inhibits 2-deoxy- (2-DG)-induced hyperphagia in rats. Biol Pharm Bull. 2001 Dec;24(12):1431-3. |
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| 15006465 | Rowland NE, Rokadia S, Green DJ, Robertson K: Relationship between anorexia and loss of uptake sites in brain of mice and rats receiving d-norfenfluramine or d-fenfluramine. Pharmacol Biochem Behav. 2004 Mar;77(3):541-6. In the first study, we show that chronic administration of neither d-norfenfluramine (D-NF; the principal metabolite of D-F) nor the serotonin (5-HT) 2C receptor agonist m-chlorophenyl-piperazine (mCPP) is associated with the development of anorectic tolerance tested using a dessert protocol. |
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| 14656323 | Paolucci E, Berretta N, Tozzi A, Bernardi G, Mercuri NB: Depression of mGluR-mediated IPSCs by in neurons of the rat substantia nigra pars compacta. Eur J Neurosci. 2003 Nov;18(10):2743-50. Similar results were obtained with alpha-methyl- and but not with 5-carboxamidotryptamine or 1-(3-chlorophenyl) piperazine. |
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| 11754579 | Brea J, Rodrigo J, Carrieri A, Sanz F, Cadavid MI, Enguix MJ, Villazon M, Mengod G, Caro Y, Masaguer CF, Ravina E, Centeno NB, Carotti A, Loza MI: New 5-HT (2A), 5-HT (2B), and 5-HT (2C) receptor antagonists: synthesis, pharmacology, 3D-QSAR, and molecular modeling of (aminoalkyl) benzo and heterocycloalkanones. J Med Chem. 2002 Jan 3;45(1):54-71. Although piperidine fragments also confer higher affinity at 5-HT (2C) receptors, only piperazine-containing ligands were selective over 5-HT (2A). |
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| 17074317 | Harada K, Aota M, Inoue T, Matsuda R, Mihara T, Yamaji T, Ishibashi K, Matsuoka N: Anxiolytic activity of a novel potent 5-HT2C receptor antagonist FR260010: a comparison with diazepam and Eur J Pharmacol. 2006 Dec 28;553(1-3):171-84. Epub 2006 Sep 28. Hyperfunction of brain (2C) (5-HT (2C)) receptor is suggested to be involved in anxiety as evidenced by the fact that a putative 5-HT (2C) receptor agonist 1-(m-chlorophenyl)-piperazine (m-CPP) causes anxiety in humans. |
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| 14769389 | Jakus R, Graf M, Juhasz G, Gerber K, Levay G, Halasz P, Bagdy G: 5-HT2C receptors inhibit and 5-HT1A receptors activate the generation of spike-wave discharges in a genetic rat model of absence epilepsy. Exp Neurol. 2003 Dec;184(2):964-72. We have determined the effects of the 5-HT (2C) receptor preferring agonist m-chlorophenyl-piperazine (m-CPP), the selective 5-HT (2C) receptor antagonist SB-242084, the selective 5-HT (1A) receptor antagonist WAY-100635, two selective re-uptake inhibitors (SSRI, fluoxetine and and their combinations in this model. |
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| 19827295 | Fiorino F, Severino B, De Angelis F, Perissutti E, Magli E, Frecentese F, Esposito A, Massarelli P, Nencini C, Viti B, Santagada V, Caliendo G: Synthesis and in vitro pharmacological evaluation of a new series of 5-HT1A 5-HT2A and 5-HT2C receptor ligands containing a norbornene nucleus. Pharmazie. 2009 Sep;64(9):555-64. A series of 4-substituted piperazine derivatives bearing a norbornene nucleus have been prepared and their affinity for 5-HT1A, 5-HT2A and 5-HT2C receptors has been evaluated. |
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| 15138762 | Lee MD, Somerville EM, Kennett GA, Dourish CT, Clifton PG: Reduced hypophagic effects of d-fenfluramine and the 5-HT2C receptor agonist mCPP in 5-HT1B receptor knockout mice. Psychopharmacology. 2004 Oct;176(1):39-49. Epub 2004 May 8. |
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| 11448452 | Porter RH, Malcolm CS, Allen NH, Lamb H, Revell DF, Sheardown MJ: Agonist-induced functional desensitization of recombinant human 5-HT2 receptors expressed in CHO-K1 cells. Biochem Pharmacol. 2001 Aug 15;62(4):431-8. The desensitization characteristics of recombinant human 5-HT (2A), 5-HT (2B), and 5-HT (2C) receptors (VSV and INI isoforms) stably expressed in CHO-K1 (Chinese hamster ovary) cells was investigated by fluorimetry. |
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| 15719229 | Hayashi A, Suzuki M, Sasamata M, Miyata K: Agonist diversity in 5-HT (2C) receptor-mediated weight control in rats. Psychopharmacology. 2005 Mar;178(2-3):241-9. Epub 2004 Oct 21. |
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| 11804612 | Hemrick-Luecke SK, Evans DC: Comparison of the potency of MDL 100,907 and SB 242084 in blocking the (5-HT)(2) receptor agonist-induced increases in rat serum concentrations: evidence for 5-HT (2A) receptor mediation of the HPA axis. Neuropharmacology. 2002 Feb;42(2):162-9. While involvement of 5-HT (1A) receptors in activation of the hypothalamic-pituitary-adrenocortical (HPA) axis is clear, the 5-HT (2) receptor subtype--5-HT (2A) or 5-HT (2C)--responsible for activation of the HPA axis by direct-acting 5-HT (2) receptor agonists has been difficult to determine due to the lack of selective pharmacologic agents. |
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| 19640898 | Miyazato M, Kaiho Y, Kamo I, Kitta T, Chancellor MB, Sugaya K, Arai Y, de Groat WC, Yoshimura N: Role of spinal serotonergic pathways in sneeze-induced urethral continence reflex in rats. Am J Physiol Renal Physiol. 2009 Oct;297(4):F1024-31. Epub 2009 Jul 29. The effect of 8-OH-DPAT and mCPP was antagonized by WAY-100635 (it), a selective 5-HT (1A) antagonist, and RS-102221 (it), a selective 5-HT (2C) antagonist, respectively. |
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| 11124393 | Schreiber R, Selbach K, Asmussen M, Hesse D, de Vry J: Effects of (1/2) receptor agonists on dark-phase food and water intake in rats. Pharmacol Biochem Behav. 2000 Oct;67(2):291-305. The following agonists were tested: ipsapirone [preferred receptor (s) and dose range in mg/kg, IP: 5-HT (1A) and 3-30, respectively], CP-94,253 (5-HT (1B); 0.3-3), TFMPP (5-HT (1B/2C); 0. 3-10), m-CPP (5-HT (2C/1B); 0.3-10), ORG 37684 (5-HT (2C); 0.3-10), BW 723C86 (5-HT (2B); 3-30) and DOI (5-HT (2A/2C); 0.3-3). |
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| 11277605 | Sanchez H, Velazquez-Martinez DN: Discriminative stimulus properties of indorenate, a 5-HT1A, 5-HT1B and 5-HT2C agonist: a study in rats. J Psychopharmacol. 2001 Mar;15(1):29-36. Generalization to the discriminative stimulus properties of INDO was observed with the 5-HT1A receptor agonist 8-OH-DPAT (1.0 mg/kg produced 90% generalization) and the 5-HT (1B/2C) receptor agonist 1-(3-trifluoromethylphenyl) piperazine (TFMPP) (3.0 mg/kg produced up to 75% generalization). |
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| 15970314 | Winter JC, Eckler JR, Rice KC, Rabin RA: Serotonergic/glutamatergic interactions: potentiation of phencyclidine-induced stimulus control by Pharmacol Biochem Behav. 2005 Jul;81(3):694-700. It was found that the selective 5-HT2C-selective antagonists, SDZ SER 082 and SB 242084, significantly, albeit only partially, blocked the effects of citalopram on PCP. |
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| 18477467 | Nonogaki K, Ohba Y, Sumii M, Oka Y: systems upregulate the expression of hypothalamic NUCB2 via 5-HT2C receptors and induce anorexia via a leptin-independent pathway in mice. Biochem Biophys Res Commun. 2008 Jul 18;372(1):186-90. Epub 2008 May 12. |
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| 12231467 | Arjona AA, Pooler AM, Lee RK, Wurtman RJ: Effect of a 5-HT (2C) agonist, dexnorfenfluramine, on amyloid precursor protein metabolism in guinea pigs. Brain Res. 2002 Sep 27;951(1):135-40. Chronic administration of mCPP (1-(m-chlorophenyl) piperazine) (2 mg/kg bid, i.p.), a 5-HT (2B/2C) agonist, for 9 days also increased CSF APP (s) levels (P <0.5) when measured 2 h after the drug's last administration; hippocampal and cortical APP (h) levels were unaffected. |
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| 15032678 | Poissonnet G, Parmentier JG, Boutin JA, Goldstein S: The emergence of selective 5-HT 2B antagonists structures, activities and potential therapeutic applications. Mini Rev Med Chem. 2004 Mar;4(3):325-30. 5-HT (2) receptors mediate a large array of physiological and behavioral functions in humans via three distinct subtypes: 5-HT (2A), 5-HT (2B) and 5-HT (2C). Indeed, four structural classes belonging to the piperazine, naphthylpyrimidine and tetrahydro-beta-carboline scaffolds were reported. |
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| 12218703 | Anderson IM, Clark L, Elliott R, Kulkarni B, Williams SR, Deakin JF: 5-HT (2C) receptor activation by m-chlorophenylpiperazine detected in humans with fMRI. Neuroreport. 2002 Aug 27;13(12):1547-51. |
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