Protein Information

Name 5 HT 5
Synonyms 5 Hydroxytryptamine receptor 5A; 5 hydroxytryptamine 5A receptor; 5 HT 5; 5 HT 5A; 5 HT 5A receptor; 5 HT5A; 5 HT5A receptor; 5 hydroxytryptamine (serotonin) receptor 5A…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
11448518 Hasuo H, Akasu T: 5-Hydroxytryptamine facilitates spatiotemporal propagation of optical signals in the hippocampal-septal pathway. Neurosci Res. 2001 Jul;40(3):265-72.

Bicuculline blocked the 5-HT-induced facilitation of the optical signal. 8-Hydroxy-di-n-propylamino tetralin (8-OH-DPAT), a selective 5-HT (1A) agonist, mimicked the facilitation of 5-HT. 1-(2-Methoxyphenyl)-4-(4-phthalimidobutyl) piperazine (NAN-190), a 5-HT (1A) antagonist, blocked the facilitation induced by 5-HT. 5-HT enhanced the amplitude of the field potential in septal slices, where the optical signals had been enhanced.
31(0,1,1,1) 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
15588097 Leopoldo M, Berardi F, Colabufo NA, Contino M, Lacivita E, Niso M, Perrone R, Tortorella V: Structure-affinity relationship study on N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides, a new class of 5-hydroxytryptamine7 receptor agents. J Med Chem. 2004 Dec 16;47(26):6616-24.

A series of N-(1,2,3,4-tetrahydronaphthalen-1-yl)-4-aryl-1-piperazinealkylamides was prepared and their affinity for serotonin (5-hydroxytryptamine, 5-HT) 5-HT7, 5-HT (1A), and 5-HT (2A) receptors was measured by in vitro binding assays.
In relation to 5-HT7 receptor affinity, receptor binding studies indicated that (i) the optimal alkyl chain length was five methylenes, (ii) an unsubstituted 1,2,3,4-tetrahydronaphthalenyl nucleus was preferred, and (iii) the substitution pattern of the aryl ring linked to the piperazine ring played a crucial role.
1(0,0,0,1) 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.

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.
6(0,0,1,1) Details
14609542 van der Vegt BJ, Lieuwes N, Cremers TI, de Boer SF, Koolhaas JM: Cerebrospinal fluid monoamine and metabolite concentrations and aggression in rats. Horm Behav. 2003 Sep;44(3):199-208.


In sharp contrast to the hypothesis and our expectation, a clear positive correlation was found between the individual level of trait-like aggressiveness and CSF concentrations of 5-HT, 5-HIAA, norepinephrine (NE), dopamine (DA), and 3,4-dihydroxyphenylacetic acid (DOPAC).
1(0,0,0,1) Details
16308184 Frampton AE, Andrews JC, Parfitt A, Jagroop IA, Mikhailidis DP, Henry JA: Does meta-chlorophenylpiperazine (mCPP) activate human platelets? . Platelets. 2006 Feb;17(1):30-6.


mCPP (meta-chlorophenylpiperazine), an agonist at serotonin (5-hydroxytryptamine, 5-HT) 5-HT2 receptors, has been used as a probe of serotonergic function.
1(0,0,0,1) Details
19345236 Lorenzi V, Carpenter RE, Summers CH, Earley RL, Grober MS: Serotonin, social status and sex change in the bluebanded goby Lythrypnus dalli. Physiol Behav. 2009 Jun 22;97(3-4):476-83. Epub 2009 Apr 2.


Males and newly sex changed fish showed a trend for higher levels of 5-HIAA and 5-HT/5-HIAA ratio than females.
1(0,0,0,1) Details
11489454 Jeong HJ, Han SH, Min BI, Cho YW: 5-HT1A receptor-mediated activation of G-protein-gated inwardly rectifying K+ current in rat periaqueductal gray neurons. Neuropharmacology. 2001 Aug;41(2):175-85.


I5-HT was mimicked by a 5-HT1A receptor selective agonist, 8-OH-DPAT, and was reversibly blocked by a 5-HT1A receptor antagonist, piperazine maleate, but not by a 5-HT2 receptor antagonist, ketanserin.
0(0,0,0,0) 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.
0(0,0,0,0) Details
11557597 Fu XW, Wang D, Pan J, Farragher SM, Wong V, Cutz E: Neuroepithelial bodies in mammalian lung express functional serotonin type 3 receptor. Am J Physiol Lung Cell Mol Physiol. 2001 Oct;281(4):L931-40.


Application of the 5-HT (5-150 microM) and 5-HT (3)-R agonist 2-methyl-5-HT (5-150 microM) induced inward currents in a concentration-dependent manner.
1(0,0,0,1) Details
15985260 Jordan S, Chen R, Koprivica V, Hamilton R, Whitehead RE, Tottori K, Kikuchi T: In vitro profile of the antidepressant candidate OPC-14523 at rat and human 5-HT1A receptors. Eur J Pharmacol. 2005 Jul 11;517(3):165-73.


This study determined the in vitro functional profile of 1-[3-[4-(3-chlorophenyl)-1-piperazinyl] propyl]-5-methoxy-3,4-dihydro-2-qui nolinone monomethanesulfonate (OPC-14523) at rat and human serotonin (5-HT) 5-HT1A receptors and binding affinity of OPC-14523 at human frontocortical 5-HT1A receptors.
1(0,0,0,1) 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.


METHODS: We investigated the decreases of plasma acylated-ghrelin level and food intake caused by cisplatin, serotonin (5-HT), 5-HT agonists, and vagotomy as well as the decrease-suppressing effects of rikkunshito and 5-HT antagonists.
1(0,0,0,1) Details
15589386 Bandoh T, Hayashi M, Ino K, Takada S, Ushizawa D, Hoshi K: Acute effect of milnacipran on the relationship between the locus coeruleus noradrenergic and dorsal raphe serotonergic neuronal transmitters. Eur Neuropsychopharmacol. 2004 Dec;14(6):471-8.


A single administration of milnacipran (60 mg/kg, s.c.) markedly decreased the levels of NA and its metabolite, 4-hydroxy-3-methoxymandelic acid (HMMA), in the locus coeruleus and the levels of, a metabolite of 5-hydroxytryptamine (5-HT), 5-hydroxyindole-3-acetic acid (5-HIAA) in the dorsal raphe nucleus.
1(0,0,0,1) Details