Protein Information

Name 5 HT 2B
Synonyms 5 hydroxytryptamine receptor 2B; 5 HT(2B); 5 HT 2B; 5 HT2B; 5 hydroxytryptamine (serotonin) receptor 2B; 5 hydroxytryptamine 2B receptor; HTR2B; Serotonin 5 HT 2B receptor…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
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.
1(0,0,0,1) 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.


DOI, a preferential 5-HT (2A) agonist (0.5-8 mg/kg) and BW 723C86, a 5-HT (2B) agonist (8 and 16 mg/kg) provoked an anxiolytic-like response in the FPT.
1(0,0,0,1) Details
11298663 Martin RS, Martin GR: Investigations into migraine pathogenesis: time course for effects of m-CPP, BW723C86 or glyceryl trinitrate on appearance of Fos-like immunoreactivity in rat trigeminal nucleus caudalis (TNC). Cephalalgia. 2001 Feb;21(1):46-52.


Therefore, we measured the effects of 5-HT2B agonists (m-CPP or BW723C86) or GTN on trigeminal nerves by quantifying Fos expression in the rat TNC. m-CPP (0.1 mg/kg, i.v.) induced time-dependent elevations in Fos-LI in the rat TNC 2 h and 8 h after injection.
1(0,0,0,1) Details
16553644 Kitazawa T, Ukai H, Komori S, Taneike T: Pharmacological characterization of 5-hydroxytryptamine-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. 5-HT applied cumulatively caused sustained contraction of the proventriculus that was not decreased by tetrodotoxin, atropine or l-nitro-arginine methylester (l-NAME). alpha-Methyl-5-HT showed the same potency as that of 5-HT, indicating the involvement of the 5-HT (2) receptor. (+/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-amino-propane (DOI), 5-methoxytryptamine 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-hydroxy-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).
1(0,0,0,1) Details
11888572 Fone KC, Topham IA: Alteration in 5-hydroxytryptamine agonist-induced behaviour following a corticosterone implant in adult rats. Pharmacol Biochem Behav. 2002 Apr;71(4):815-23.


The elevation in plasma corticosterone 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 corticosterone 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 corticosterone was abolished by corticosterone treatment.
1(0,0,0,1) Details
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.


To clarify the role of spinal serotonergic mechanisms in preventing stress urinary incontinence (SUI) during sneezing, we investigated the effect of intrathecal (it) application of 8-OH-DPAT (a 5-HT (1A) agonist), mCPP (a 5-HT (2B/2C) agonist), and fluoxetine (a serotonin reuptake inhibitor) using a rat model that can examine the neurally evoked continence reflex during sneezing.
1(0,0,0,1) Details
12892833 Zanoveli JM, Nogueira RL, Zangrossi H Jr: Serotonin 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.


In these two test conditions, intra-dorsal periaqueductal gray injection of the endogenous agonist serotonin or the 5-HT (2B/2C) receptor agonist m-chlorophenylpiperazine (mCPP) enhanced inhibitory avoidance, suggesting an anxiogenic effect.
1(0,0,0,1) Details
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-5-HT (alpha-methyl-5-hydroxytryptamine) 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.
0(0,0,0,0) Details
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 5-HT (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.
0(0,0,0,0) Details
12716945 Zhang ZW: Serotonin induces tonic firing in layer V pyramidal neurons of rat prefrontal cortex during postnatal development. J Neurosci. 2003 Apr 15;23(8):3373-84.


The excitatory effects of 5-HT at younger ages were attributed to 5-HT2A receptors because the effects were mimicked by the 5-HT2 agonist alpha-methyl-5-HT but not by the 5-HT3 agonist 1-(m-chlorophenyl)-biguanide, nor by the 5-HT2B/2C agonist 1-(3-chlorophenyl) piperazine, and were blocked by the 5-HT2A antagonists ketanserin and alpha-phenyl-1-(2-phenylethyl)-4-piperidinemethanol.
0(0,0,0,0) Details
16165167 Walker EA, Kohut SJ, Hass RW, Brown EK Jr, Prabandham A, Lefever T: Selective and nonselective serotonin 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.


Selective 5-HT (2B/2C) antagonist SB206,553 blocked both MK212- and mCPP-induced conditioned taste aversion although selective 5-HT (2B/2C) antagonist SB200,646 only blocked mCPP-induced conditioned taste aversion.
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 imipramine-induced hyperglycemia in mice. Horm Metab Res. 2003 Sep;35(9):511-6.


Imipramine 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
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-fluoro-indol-1-yl)-1-methyl-ethylamine fumarate (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.
0(0,0,0,0) Details
16710314 McCreary AC, Glennon JC, Ashby CR Jr, Meltzer HY, Li Z, Reinders JH, Hesselink MB, Long SK, Herremans AH, van Stuivenberg H, Feenstra RW, Kruse CG: SLV313 (1-(2,3-dihydro-benzo [1,4] dioxin-5-yl)-4- [5-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-piperazine monohydrochloride): a novel dopamine D2 receptor antagonist and 5-HT1A receptor agonist potential antipsychotic drug. Neuropsychopharmacology. 2007 Jan;32(1):78-94. Epub 2006 May 17.

0(0,0,0,0) Details
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 serotonin 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.

Significant selectivity at the 5-HT (2B) receptor vs 5-HT (2C) was observed with 1-1 [(1-oxo-1,2,3,4-tetrahydro-3-naphthyl) methyl]-4-[3-(p-fluorobenzoyl) pro pyl] piperazine (more than 100-fold higher).
88(1,1,1,8) Details
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.
81(1,1,1,1) Details
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.
35(0,1,1,5) Details
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 dopamine (D (1), D (2), D (4)) and serotonin (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 dopamine 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.
32(0,1,1,2) Details
12231467 Arjona AA, Pooler AM, Lee RK, Wurtman RJ: Effect of a 5-HT (2C) serotonin 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.
31(0,1,1,1) Details
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.

Indeed, four structural classes belonging to the piperazine, indole, naphthylpyrimidine and tetrahydro-beta-carboline scaffolds were reported.
5(0,0,0,5) Details
12885436 Castro L, Athanazio R, Barbetta M, Ramos AC, Angelo AL, Campos I, Varjao B, Ferreira H, Fregoneze J, de Castro e Silva E: Central 5-HT2B/2C and 5-HT3 receptor stimulation decreases salt intake in sodium-depleted rats. Brain Res. 2003 Aug 15;981(1-2):151-9.

4(0,0,0,4) Details
12603368 Johnson KW, Nelson DL, Dieckman DK, Wainscott DB, Lucaites VL, Audia JE, Owton WM, Phebus LA: Neurogenic dural protein extravasation induced by meta-chlorophenylpiperazine (mCPP) involves nitric oxide and 5-HT2B receptor activation. Cephalalgia. 2003 Mar;23(2):117-23.

4(0,0,0,4) Details
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.


METHODS: Male rats, habituated to clear Perspex behavioural observation boxes, were pretreated with antagonists with mixed selectivity for OX1, OX2, 5-HT2B and 5-HT2C receptor subtypes prior to the administration of orexin-A and the intense grooming response elicited by this peptide assessed.
4(0,0,0,4) Details
17584957 Papageorgiou A, Denef C: Stimulation of growth hormone release by 5-hydroxytryptamine (5-HT) 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-HT; 5-carboxytryptamine (agonist at 5-HTR1, -5, and -7); tryptamine (preferential 5-HTR7 agonist); and the selective 5-HTR1B agonist CP93129 but not the 5-HTR1A agonists 7-(dipropylamino) tetralin-1-ol-8-hydroxy-2-(di-n-propylamino) tetralin and the 5-HTR1B/D agonist sumatriptan.
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.
4(0,0,0,4) Details
12062579 Castro L, Maldonado I, Campos I, Varjao B, Angelo AL, Athanazio RA, Barbetta MC, Ramos AC, Fregoneze JB, De Castro e Silva E: Central administration of mCPP, a serotonin 5-HT (2B/2C) agonist, decreases water intake in rats. Pharmacol Biochem Behav. 2002 Jul;72(4):891-8.

In the present study, we investigated in rats the effect of third ventricle injections of 1-(3-chlorophenyl) piperazine (mCPP), a 5-HT (2) receptor agonist, on water intake induced by three different physiological stimuli: fluid deprivation, acute salt load and hypovolemia.
2(0,0,0,2) Details
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-methoxytryptamine (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.
2(0,0,0,2) 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.
The proejaculatory effect of m-CPP was also attenuated by ketanserin (0.3 and 1.0 mg/kg, i.p.), a 5-HT (2A) receptor antagonist, whereas SB204741 (0.1 and 0.3 mg/kg, i.p.), a selective 5-HT (2B) receptor antagonist, significantly potentiated the m-CPP-induced ejaculatory response.
2(0,0,0,2) Details
11124393 Schreiber R, Selbach K, Asmussen M, Hesse D, de Vry J: Effects of serotonin (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 5-HT 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
15892984 Kubera M, Maes M, Kenis G, Kim YK, Lason W: Effects of serotonin and serotonergic agonists and antagonists on the production of tumor necrosis factor alpha and interleukin-6. Psychiatry Res. 2005 Apr 30;134(3):251-8.


The specific aims were to examine the effects of 5-HT, p-chlorophenylalanine (PCPA), a 5-HT depleting agent, flesinoxan, a 5-HT (1A) agonist, m-chlorophenylpiperazine (mCPP), a 5-HT (2B/2C) agonist, and ritanserin, a 5-HT (2A/2C) antagonist, on the production of the above cytokines.
1(0,0,0,1) Details
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 pharmacology of several commonly described 5-hydroxytryptamine (5-HT)(2C) receptor agonists was investigated in vivo and in vitro at rat 5-HT (2A), 5-HT (2B), and 5-HT (2C) receptors.
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.
1(0,0,0,1) Details
18582863 Kimura Y, Naitou Y, Wanibuchi F, Yamaguchi T: 5-HT (2C) receptor activation is a common mechanism on proerectile effects of apomorphine, oxytocin and melanotan-II in rats. Eur J Pharmacol. 2008 Jul 28;589(1-3):157-62. Epub 2008 May 24.


In this study, in order to clarify these matters, we examined the effects of a selective 5-HT (2B)/5-HT (2C) receptors antagonist, 1-(1-methylindol-5-yl)-3-(3-pyridyl) urea (SB200646) and a selective 5-HT (2C) receptor antagonist, 6-chloro-5-methyl-1-[6-(2-methylpyridin-3-yloxy) pyridin-3-yl carbamoyl] indoline (SB242084) on penile erections induced by a dopamine receptor agonist, 10, 11-dihydroxyaporphine (apomorphine), oxytocin, or a melanocortin receptor agonist, melanotan-II (MT-II) in rats.
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 dopamine 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 serotonin (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.
1(0,0,0,1) Details
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.
We investigated the effects of the selective 5-HT (2A) antagonists, MDL 100,907 and ketanserin, the selective 5-HT (2B) antagonists, LY 202146 and LY 266097, the 5-HT (2B/2C) antagonist, SB 206553, and the selective 5-HT (2C) antagonist, SB 242084 on m-CPP-induced hypolocomotion and spontaneous locomotor activity in mice.
1(0,0,0,1) Details
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 calcium fluorimetry.
2(0,0,0,2) 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.


Experiment 1 assessed the effects of intra-PAG infusions of the 5-HT2B/2C receptor agonist mCPP (0, 0.03, 0.1 or 0.3 nmol/0.1 microl) on the behaviour of mice exposed to the elevated plus-maze.
2(0,0,0,2) Details
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.


The present study investigated the effects of the 5-HT (2B/2C) receptor agonist mCPP bilaterally microinjected into the dorsal hippocampus (DH: 0, 0.3, 1.0 or 3.0nmol/0.2microl), the ventral hippocampus (VH: 0, 0.3, 1.0 or 3.0nmol/0.2microl) or the amygdaloid complex (0, 0.15, 0.5, 1.0 or 3.0nmol/0.1microl) in mice exposed to the elevated plus-maze (EPM).
1(0,0,0,1) Details
11595362 Houston GC, Papadakis NG, Carpenter TA, Hall LD, Mukherjee B, James MF, Huang CL: Mapping of brain activation in response to pharmacological agents using fMRI in the rat. Magn Reson Imaging. 2001 Sep;19(7):905-19.


The effects of dizocilpine (MK-801) an N-methyl-D-aspartate receptor antagonist and m-chlorophenylpiperazine (mCPP), a 5-HT (2b/2c)-receptor agonist on rat brain activity were investigated over a time interval of about 1 h and the results were compared to published glucose utilisation and cerebral blood flow data.
1(0,0,0,1) 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.


To characterise the possible role, 5-HT (2B) and 5-HT (2C) receptors play in m-CPP-induced self-grooming, subtype-selective receptor antagonists were used. m-CPP significantly increased the amount of self-grooming in male Sprague-Dawley rats.
1(0,0,0,1) Details
12585687 Meneses A: Involvement of 5-HT (2A/2B/2C) receptors on memory formation: simple agonism, antagonism, or inverse agonism?. Cell Mol Neurobiol. 2002 Dec;22(5-6):675-88.

However, both drugs significantly and differentially antagonized the memory impairments induced by 1-(3-chlorophenyl) piperazine (mCPP), 1-naphtyl-piperazine (1-NP), mesulergine, or N-(3-trifluoromethylphenyl) piperazine (TFMPP). 3.
It is suggested that 5-HT (2B/2C) receptors might be involved on memory formation probably mediating a suppressive or constraining action.
1(0,0,0,1) Details