| Name | 5 HT1B |
|---|---|
| Synonyms | 5 HT 1B; S12; 5 HT 1D beta; 5 HT1B; 5 HT1DB; 5 hydroxytryptamine (serotonin) receptor 1B; 5 hydroxytryptamine 1B receptor; HTR1B… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 11323141 | Zhang Y, Yang Z, Gao X, Wu G: The role of 5-hydroxytryptamine1A and 5-hydroxytryptamine1B receptors in modulating spinal nociceptive transmission in normal and carrageenan-injected rats. Pain. 2001 May;92(1-2):201-11. These data suggest that 5-HT1A and 5-HT1B receptor subtypes mediate the facilitatory effect of on nociceptive processing in the spinal cord of rats. |
2(0,0,0,2) | Details |
| 11006953 | Heidenreich BA, Napier TC: Effects of serotonergic 5-HT1A and 5-HT1B ligands on ventral pallidal neuronal activity. Neuroreport. 2000 Sep 11;11(13):2849-53. |
2(0,0,0,2) | Details |
| 11070185 | Shaw AM, Bunton DC, Brown T, Irvine J, MacDonald A: Regulation of sensitivity to in pulmonary supernumerary but not conventional arteries by a 5-HT (1D)-like receptor. Eur J Pharmacol. 2000 Nov 10;408(1):69-82. The selective 5-HT (2) receptor antagonist ritanserin produced insurmountable antagonism of concentration-response curves in both arteries, whereas the 5-HT (1B/1D) receptor antagonist N-[4-methoxy-3-(4-methyl-1-piperazinyl) phenyl]-2'-methyl-4'(5-methyl- 1,2,4-oxadiazol-3-yl [1,1,-biphenyl]-4-carboxamide hydrochloride (GR127935) produced much greater antagonism in supernumerary arteries. Neither the selective 5-HT (1D) receptor antagonist (1-(3-chlorophenyl)-4-[3, 3-diphenyl (2-(S,R) hydroxypropanyl) piperazine] hydrochloride (BRL15572) nor the 5-HT (1B) receptor antagonist (2,3,6, 7-tetrahydro-1'-methyl-5-[2'methyl-4'5-(methyl-1,2,4-oxadiazol-3-y l) biphenyl-4-carbonyl] furo [2,3-f] -3-spiro-4'-piperidine hydrochloride (SB224289) antagonised concentration-response curves induced by or (1)-receptor-selective agonists. |
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 |
| 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). |
2(0,0,0,2) | Details |
| 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 are consistent with involvement of the dopaminergic and systems, in particular activation of 5-HT1A and 5-HT1B receptor subtypes, in mediation of the conditioned or secondary reinforcing properties of 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. |
1(0,0,0,1) | Details |
| 18996171 | Ita ML, Cortes Mdel C, Valencia J, Eguibar JR: Activation of 5-HT1-receptors decreased gripping-induced immobility episodes in taiep rats. Neurosci Lett. 2009 Jan 9;449(2):147-50. Epub 2008 Oct 30. In male 8-month-old taiep rats we have studied the effect of systemic administration of serotonergic autoreceptor agonists and antagonists on gripping-induced IEs. 8--2-(di-n-propylamino) tetraline hydrobromide (8-OH-DPAT), a 5-HT (1A) agonist, and 3-trifluoromethylphenylpiperazine hydrochloride (TFMPP), a 5-HT (1B) agonist, produce a significant decrease in the frequency and mean duration of IEs. Systemic administration of spiperone and 1-(2-methoxyphenyl)-4 [4-(2-phthalimido) butyl] piperazine hydrobromide (NAN-190), (1) antagonists, increase IEs and their mean duration. |
1(0,0,0,1) | Details |
| 16153839 | Wyman PA, Marshall HR, Flynn ST, King RJ, Thompson M, Smith PW, Hadley MS, Price GW, Scott CM, Dawson LA: Identification of a potent and selective 5-HT1B receptor antagonist. . Bioorg Med Chem Lett. 2005 Nov 1;15(21):4708-12. An SAR study around the mixed 5-HT1ABD receptor antagonist SB-272183 found that introduction of cis-2,6-dimethyl substitution onto the piperazine ring was a key structural change, which imparted a combination of both excellent selectivity over the 5-HT1A and 5-HT1D receptors and low intrinsic activity. |
2(0,0,0,2) | Details |
| 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. Both BRL 15572 (a 5-HT (1D) receptor antagonist) and GR 55562 (a 5-HT (1B) receptor antagonist) only partially inhibited this action. |
1(0,0,0,1) | 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. We previously reported that fluvoxamine, a selective reuptake inhibitor, together with pharmacological inactivation of 5-HT2C receptors exert feeding suppression through activation of 5-HT1B receptors in mice. |
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. Moreover, pre-treatment of pindolol (10 mg/kg, i.p., a beta-adrenoceptors blocker/5-HT (1A/1B) receptor antagonist), 4-(2'-methoxy-phenyl)-1-[2'-(n-2''-pyridinyl)-p-iodobenzamino-] ethyl-piper azine (p-MPPI, 1 mg/kg, s.c., a selective 5-HT (1A) receptor antagonist), or 1-(2-(1-pyrrolyl)-phenoxy)-3-isopropylamino- (isamoltane, 2.5 mg/kg, i.p., a 5-HT (1B) receptor antagonist) was found to prevent the effect of (10 mg/kg) in forced swimming test. |
1(0,0,0,1) | Details |
| 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. |
1(0,0,0,1) | Details |
| 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. An anorectic dose of the 5-HT (1B/2C) receptor agonist m-chlorophenylpiperazine (mCPP; 3 mg/kg s.c.) was used to compare BOLD contrast fMRI with expression of the c-Fos protein. mCPP was administered to rats, which were then anaesthetised and perfused with fixative 90 min later to allow immunohistochemistry. |
1(0,0,0,1) | Details |
| 18469535 | Farrell MS, Gilmore K, Raffa RB, Walker EA: Behavioral characterization of serotonergic activation in the flatworm Planaria. Behav Pharmacol. 2008 May;19(3):177-82. This study characterized the behavioral and locomotor effects of a 5-HT1A agonist, a 5-HT1B/2C agonist, and a 5-HT1A antagonist to examine the role of receptor activation in this species. |
1(0,0,0,1) | Details |
| 11965359 | Popova NK, Amstislavskaya TG: Involvement of the 5-HT (1A) and 5-HT (1B) serotonergic receptor subtypes in sexual arousal in male mice. Psychoneuroendocrinology. 2002 Jul;27(5):609-18. |
1(0,0,0,1) | Details |
| 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. Effects of TFMPP, alone and with the 5-HT (1A) receptor antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-2-pyridinyl-cyclohexanecarboxamine (WAY 100635), the 5-HT (1B) receptor antagonist N-[4-methoxy-3-(4-methyl-1-piperazinyl) phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-1,1'-biphenyl-4-carbo xamide (GR 127935) or the 5-HT2C receptor antagonist 6-chloro-5-methyl-1-[[2-(2-methylpyrid-3-yloxy) pyrid-5-yl] carbamoyl] indoli ne (SB 242084) and of WAY 161503 alone and with SB 242084 on locomotor activity were also assessed. |
1(0,0,0,1) | Details |
| 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. Agonists acting at the serotonin-1B receptor (5-HT1BR) and 5-HT2CR have been reported to potentiate and block, respectively, the discriminative stimulus effects of cocaine. |
1(0,0,0,1) | Details |
| 15577454 | Porcu P, Grant KA: Discriminative stimulus effects of in rats using a three-choice -midazolam-water discrimination. Behav Pharmacol. 2004 Dec;15(8):555-67. Substitution tests were conducted following administration of GABAA-positive modulators, noncompetitive antagonists, 5-HT1B agonists and |
1(0,0,0,1) | Details |
| 11948242 | Tohyama Y, Yamane F, Fikre Merid M, Blier P, Diksic M: Effects of serotine receptors agonists, TFMPP and CGS12066B, on regional synthesis in the rat brain: an autoradiographic study. J Neurochem. 2002 Mar;80(5):788-98. The observed effects in the 7-day treatment could also be related to actions through the postsynaptic 5-HT (1B) sites and/or other receptors since this compounds have limited selectivity. |
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 |
| 11853106 | Haleem DJ, Saify ZS, Siddiqui S, Batool F, Haleem MA: Pre- and postsynaptic responses to 1-(1-naphthylpiperazine) following adaptation to stress in rats. Prog Neuropsychopharmacol Biol Psychiatry. 2002 Jan;26(1):149-56. The results are discussed in the context of an increase in the effectiveness of postsynaptic 5-HT-1A and 5-HT-1B receptors and a decrease in the effectiveness of presynaptic 5-HT-1A (somatodendritic) and 5-HT-1B (terminal) receptors following adaptation to stress. |
1(0,0,0,1) | Details |
| 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. Here, we show that systemic administration of m-chlorophenylpiperazine (mCPP), a 5-HT1B/2C receptor agonist, significantly increased the expression of hypothalamic NUCB2 in wild-type mice. |
1(0,0,0,1) | Details |
| 15380867 | Landry ES, Guertin PA: Differential effects of 5-HT1 and 5-HT2 receptor agonists on hindlimb movements in paraplegic mice. Prog Neuropsychopharmacol Biol Psychiatry. 2004 Sep;28(6):1053-60. Altogether, these results demonstrate that 5-HT (2A/2C) receptor agonists promote locomotion while 5-HT (1B) and 5-HT (2B/2C) receptor agonists interfere with locomotor genesis in the hindlimbs of complete paraplegic mice. |
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. |
0(0,0,0,0) | Details |
| 15374751 | Dias Elpo Zomkowski A, Oscar Rosa A, Lin J, Santos AR, Calixto JB, Lucia Severo Rodrigues A: Evidence for serotonin receptor subtypes involvement in antidepressant like-effect in the mouse forced swimming test. Brain Res. 2004 Oct 15;1023(2):253-63. Pretreatment with p-chlorophenylalanine methyl ester (PCPA; 100 mg/kg, intraperitoneally (i.p.), an inhibitor of synthesis, for 4 consecutive days), methysergide (5 mg/kg, i.p., a antagonist), pindolol (32 mg/kg, i.p., a 5-HT (1A/1B) receptor/beta-adrenoceptor antagonist), N-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-N-(2-pyridynyl) cyclohexanec arboxamide (WAY 100635; 0.3 mg/kg, subcutaneously (s.c.), a selective 5-HT (1A) receptor antagonist), 1-(2-methoxyphenyl)-4 [-(2-phthalimido) butyl] piperazine) -190; 0.5 mg/kg, i.p., a 5-HT (1A) receptor antagonist), 1-(2-(1-pyrrolyl)-phenoxy)-3-isopropylamino- (isamoltane; 2.5 mg/kg, i.p., a 5-HT (1B) receptor antagonist), cyproheptadine (3 mg/kg, i.p., a 5-HT (2) antagonist) or ketanserin (5 mg/kg, i.p., a 5-HT (2A/2C) receptor antagonist), but not with (2 mg/kg, i.p., a beta-adrenoceptor antagonist), prevented the effect of (10 mg/kg, i.p.) in the FST. |
0(0,0,0,0) | Details |
| 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. |
0(0,0,0,0) | Details |
| 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). |
0(0,0,0,0) | Details |
| 15072840 | Moloney GP, Garavelas A, Martin GR, Maxwell M, Glen RC: Synthesis and serotonergic activity of variously substituted (3-amido) phenylpiperazine derivatives and benzothiophene-4-piperazine derivatives: novel antagonists for the vascular 5-HT1B receptor. Eur J Med Chem. 2004 Apr;39(4):305-21. |
115(1,2,2,5) | Details |
| 12163345 | Rodriguez-Manzo G, Lopez-Rubalcava C, Hen R, Fernandez-Guasti A: Participation of 5-HT (1B) receptors in the inhibitory actions of on masculine sexual behaviour of mice: pharmacological analysis in 5-HT (1B) receptor knockout mice. Br J Pharmacol. 2002 Aug;136(8):1127-34. 1 The role of the (1B) (5-HT (1B)) receptor subtype in masculine sexual behaviour in mice was analysed in both 5-HT (1B) receptor knockout (KO (1B)) and wild-type (WT) animals. 2 Comparison of male copulatory behaviour of WT and KO (1B) strains revealed that KO (1B) mice become interested earlier in sexual behaviour, but require more stimulation to achieve ejaculation than its corresponding WT strain. 3 The pharmacological manipulation of male sexual activity in the WT strain showed that the precursor the 5-HT (1B) agonist (1-(m-trifluoromethylphenyl) piperazine (TFMPP) and the (1A) (5-HT (1A)) receptor agonist 8--2-di-n-propylamino-tetralin (8-OH-DPAT) all inhibited male copulatory behaviour in mice. 4 In KO (1B) mice, TFMPP lacked an effect, exerted a mild inhibitory effect while 8-OH-DPAT provoked only a tendency towards a reduction in the percentage of animals that achieved ejaculation. |
84(1,1,1,4) | Details |
| 11504649 | McCort G, Hoornaert C, Aletru M, Denys C, Duclos O, Cadilhac C, Guilpain E, Dellac G, Janiak P, Galzin AM, Delahaye M, Guilbert F, O'Connor S: Synthesis and SAR of 3- and 4-substituted quinolin-2-ones: discovery of mixed 5-HT (1B)/5-HT (2A) receptor antagonists. Bioorg Med Chem. 2001 Aug;9(8):2129-37. Quinolin-2-ones bearing a heteroaryl-piperazine linked by a two carbon chain at the 3- or 4-position were synthesised and evaluated as mixed 5-HT (1B)/5-HT (2A) receptor antagonists. |
83(1,1,1,3) | Details |
| 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). |
83(1,1,1,3) | 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. 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). |
82(1,1,1,2) | Details |
| 16032412 | Troelsen KB, Nielsen EO, Mirza NR: Chronic treatment with duloxetine is necessary for an anxiolytic-like response in the mouse zero maze: the role of the serotonin transporter. Psychopharmacology. 2005 Oct;181(4):741-50. Epub 2005 Sep 29. In mice treated chronically, (a) the hypothermic response to (5-HT) 1A and 5-HT1B receptor ligands, 8--2-(di-n-propylamino) tetralin (8-OHDPAT) and m-chlorophenyl piperazine (mCPP), respectively, was assessed and (b) serotonin transporter (SERT) and transporter (NET) densities in the cortex and hippocampus, respectively, were determined. |
81(1,1,1,1) | Details |
| 11888550 | Millan MJ, Newman-Tancredi A, Lochon S, Touzard M, Aubry S, Audinot V: Specific labelling of 5-HT (1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H] GR125,743. Pharmacol Biochem Behav. 2002 Apr;71(4):589-98. In competition binding studies, affinities were determined for 15 chemically diverse 5-HT (1B) agonists, including 2-[5-[3-(4-methylsulphonylamino) benzyl-1,2,4-oxadiazol-5-yl]-1H-indole-3-y l] ethylamine (L694,247; pK (i), 10.4), 5-carboxamidotryptamine (5-CT; 9.7), 3-[3-(2-dimethylamino-ethyl)-1H-indol-6-yl]-N-(4-methoxybenzyl) acrylamide (GR46,611; 9.6), 5-methoxy-3-(1,2,5,6-tetrahydro-4-pyridinyl)-1H-indole (RU24,969; 9.5), dihydroergotamine (DHE; 8.6), 5-H-pyrrolo [3,2-b] pyridin-5-one,1,4-dihydro-3-(1,2,3,6-tetrahydro-4-pyridi nyl (CP93,129; 8.4), anpirtoline (7.9), (7.4), 1-[2-(3-fluorophenyl) ethyl]-4-[3-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl] pro pyl] piperazine (L775,606; 6.4) and (minus sign)-1 (S)-[2-[4-(4-methoxyphenyl) piperazin-1-yl] ethyl]-N-methyl-3,4-dihyd ro-1H-2-benzopyran-6-carboxamide (PNU109,291; <5.0). |
37(0,1,1,7) | Details |
| 14744615 | Villalon CM, Centurion D, Willems EW, Arulmani U, Saxena PR, Valdivia LF: 5-HT1B receptors and alpha 2A/2C-adrenoceptors mediate external carotid vasoconstriction to dihydroergotamine. Eur J Pharmacol. 2004 Jan 26;484(2-3):287-90. This response was: (1) partly blocked in dogs pretreated intravenously with the antagonists SB224289 (5-HT (1B); 2,3,6,7-tetrahydro-1'-methyl-5-[2'-methyl-4' (5-methyl-1,2,4-oxadiazol-3-yl) biphenyl-4-carbonyl] furo [2,3-f] -3-spi ro-4'-piperidine hydrochloride), rauwolscine (alpha (2)), BRL44408 (alpha (2A); 2-[2H-(1-methyl-1,3-dihydroisoindole) methyl]-4,5-dihydroimidazole) or MK912 (alpha (2C); (2S,12bS)-1'3'-dimethylspiro (1,3,4,5',6,6',7,12b-octahydro-2Hbenzo [b] furo [ 2,3-a] quinazoline)-2,4'-pyrimidin-2'-one); (2) markedly blocked after SB224289 plus rauwolscine; and (3) unaffected after BRL15572 (5-HT (1D); 1-(3-chlorophenyl)-4-[3,3-diphenyl (2-(S,R) hydroxypropanyl) piperazine] hydrochloride) or imiloxan (alpha (2B)). |
34(0,1,1,4) | Details |
| 11216445 | Villalon CM, Centurion D, Sanchez-Lopez A, De Vries P, Saxena P: receptors mediating external carotid vasoconstriction in vagosympathectomized dogs. Zhongguo Yao Li Xue Bao. 1999 Dec;20(12):1057-67. With the advent of subtype-selective antagonists it was subsequently shown that external carotid vasoconstriction to and is dose-dependently antagonized by the selective 5-HT1B receptor antagonist SB224289 (2,3,6,7-tetrahydro-1'-methyl-5-[2'-methyl-4' (5-methyl-1,2,4-oxadiazol-3-yl) biphenyl-4-carbonyl] furo [2,3-f] -3-spiro-4'-piperidine hydrochloride), whereas the selective 5-HT1D receptor antagonist BRL15572 (1-(3-chlorophenyl)-4-[3,3-diphenyl (2-(S,R) hydroxypropanyl) piperazine] hydrochloride) was ineffective. |
34(0,1,1,4) | Details |
| 20088516 | Nugiel DA, Krumrine JR, Hill DC, Damewood JR Jr, Bernstein PR, Sobotka-Briner CD, Liu J, Zacco A, Pierson ME: De novo design of a picomolar nonbasic 5-HT (1B) receptor antagonist. . J Med Chem. 2010 Feb 25;53(4):1876-80. We used a known 5-HT (1B) antagonist template as our starting point and focused on replacing the piperazine moiety. |
34(0,1,1,4) | Details |
| 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. |
33(0,1,1,3) | Details |
| 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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| 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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| 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. 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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| 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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| 11093763 | Morikawa H, Manzoni OJ, Crabbe JC, Williams JT: Regulation of central synaptic transmission by 5-HT (1B) auto- and heteroreceptors. Mol Pharmacol. 2000 Dec;58(6):1271-8. N-(3-Trifluoromethylphenyl) piperazine, a 5-HT (1B) receptor agonist, potently inhibited 5-HT (1A) receptor-mediated slow inhibitory postsynaptic potentials (IPSPs) in the dorsal raphe of wild-type but not knockout mice. |
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| 11220775 | Smith BN, Sollars PJ, Dudek FE, Pickard GE: Serotonergic modulation of retinal input to the mouse suprachiasmatic nucleus mediated by 5-HT1B and 5-HT7 receptors. J Biol Rhythms. 2001 Feb;16(1):25-38. As previously described in the hamster, a mixed 5-HT (1A/1B) receptor agonist, 1-[3-(trifluoromethyl) phenyl]-piperazine hydrochloride (TFMPP), reduced the amplitude of glutamatergic excitatory postsynaptic currents (EPSCs) evoked by selectively stimulating the optic nerve of wild-type mice. |
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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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| 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. Serotonergic 5-HT2C and 5-HT1B receptors mediate inhibitory controls of eating. |
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| 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. |
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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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| 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. Compounds that stimulate 5-HT2C and/or 5-HT1B receptors induce hypophagia, but the relative role of these receptors in the control of feeding behaviour remains to be unequivocally demonstrated. |
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| 17392733 | Lee JJ, Hahm ET, Lee CH, Cho YW: Serotonergic modulation of GABAergic and glutamatergic synaptic transmission in mechanically isolated rat medial preoptic area neurons. Neuropsychopharmacology. 2008 Jan;33(2):340-52. Epub 2007 Mar 28. (5-hydroxytryptamine, inhibits sexual behavior via effects in the MPOA, where there are high densities of 5-HT (1A) and 5-HT (1B) receptor subtypes. Serotonergic inhibition of mIPSC frequency was mimicked by (+/-)-8--2-dipropylaminotetralin hydrobromide, a specific 5-HT (1A) receptor agonist, and blocked by 1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide, a specific 5-HT (1A) receptor antagonist. 6--7-nitroquinoxaline-2,3-dione completely blocked spontaneous glutamatergic miniature excitatory postsynaptic currents (mEPSCs) in the MPOA. |
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| 17584957 | Papageorgiou A, Denef C: Stimulation of growth hormone release by in cultured rat anterior pituitary cell aggregates: evidence for mediation by 5-HT2B, 5-HT7, 5-HT1B, and ketanserin-sensitive receptors. Endocrinology. 2007 Sep;148(9):4509-22. Epub 2007 Jun 21. Basal GH release was stimulated by the 5-HTR2 agonists 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane, m-chlorophenyl piperazine, and alpha-methyl 5-carboxytryptamine (agonist at 5-HTR1, -5, and -7); (preferential 5-HTR7 agonist); and the selective 5-HTR1B agonist CP93129 but not the 5-HTR1A agonists 7-(dipropylamino) tetralin-1-ol-8--2-(di-n-propylamino) tetralin and the 5-HTR1B/D agonist |
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| 15450869 | Lehr T, Schipp R: An antagonistic receptor system in the auricles of the systemic heart complex of Sepia officinalis L. (Cephalopoda) shows 5-HT1 and 5-HT4 subtype properties. Comp Biochem Physiol C Toxicol Pharmacol. 2004 Jun;138(2):213-9. In pharmacological bioassays on isolated ring-shaped auricle preparations of Sepia officinalis, the action of the specific agonists 8-OH-DPAT (5-HT1a), CP-93129 (5-HT1b), TFMPP (5-HT1b) and RS-67333 (5-HT4) on these autonomously contractile compartments was studied. 8-OH-DPAT and CP-93129 induced mainly positive effects on frequency and tone on the isotonically suspended auricles. |
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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. In the present group of experiments, we evaluate the role of 5-HT1A, 5-HT1B and 5-HT2A receptors in mCPP-induced hyperactivity in 5-HT2C KO mice. |
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| 12522075 | Mlinar B, Falsini C, Corradetti R: Pharmacological characterization of 5-HT (1B) receptor-mediated inhibition of local excitatory synaptic transmission in the CA1 region of rat hippocampus. Br J Pharmacol. 2003 Jan;138(1):71-80. The aim of the present work was the pharmacological characterization of the receptor involved in this action. 2 Poly-epscs, evoked by electrical stimulation of the stratum radiatum and recorded in whole-cell voltage-clamp from CA1 pyramidal neurones, were studied in mini-slices of the CA1 region under pharmacological block of (A), (B), and 5-HT (1A) receptors. 3 The 5-HT (1B) receptor selective agonist 1,4-dihydro-3-(1,2,3,6-tetrahydro-4-pyridinyl)-5H-pyrrolo [3,2-b] pyridin-5- one dihydrochloride (CP 93129) inhibited poly-epscs (EC (50)=55 nM), an effect mimicked by the 5-HT (1B) ligands 5-carboxamidotryptamine (5-CT; EC (50)=14 nM) and methylergometrine (EC (50)=78 nM), but not by 1-(3-chlorophenyl) piperazine dihydrochloride (mCPP; 10 micro M) or 7-trifluoromethyl-4 (4-methyl-1-piperazinyl)-pyrrolo [1,2-a] quinoxaline dimaleate (CGS 12066B; 10 micro M). 4 The effects of CP 93129 and 5-CT were blocked by the selective 5-HT (1B) receptor antagonist 3-[3-(dimethylamino) propyl]-4-hydroxy-N-[4-(4-pyridinyl) phenyl] benzamide dihydrochloride (GR 55562; K (B) approximately 100 nM) and by cyanopindolol (K (B)=6 nM); methiothepin (10 micro M) and dihydroergotamine (1 micro M). |
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| 18339980 | Dennis RL, Chen ZQ, Cheng HW: Serotonergic mediation of aggression in high and low aggressive chicken strains. Poult Sci. 2008 Apr;87(4):612-20. At 24 wk of age, the subordinate of each pair received a daily i.p. injection of NAN-190 (0.5 mg/kg, a 5-HT1A antagonist), GR-127935 (0.5 mg/kg, a 5-HT1B antagonist), or saline (control) for 5 consecutive days. |
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