Protein Information

Name 5 HT4
Synonyms 5 HT4; serotonin receptor; 5 hydroxytryptamine 4 receptor; 5 hydroxytryptamine receptor 4; 5 HT 4; 5 HT4R; 5 hydroxytryptamine (serotonin) receptor 4; Cardiac 5 HT4 receptor…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
12801225 Berque-Bestel I, Soulier JL, Giner M, Rivail L, Langlois M, Sicsic S: Synthesis and characterization of the first fluorescent antagonists for human 5-HT4 receptors. J Med Chem. 2003 Jun 19;46(13):2606-20.

Fluorescent antagonists for human 5-HT (4) receptors were synthesized based on ML10302 1, a potent 5-HT (4) receptor agonist and on piperazine analogue 2.
83(1,1,1,3) Details
15450869 Lehr T, Schipp R: An antagonistic 5-HT 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.

3(0,0,0,3) Details
16728720 Lau DH, Thompson CS, Bellringer JF, Thomas PJ, Mumtaz FH, Morgan RJ, Mikhailidis DP: Doxazosin and serotonin (5-HT) receptor (1A, 2A, and 4) antagonists inhibit 5-HT-mediated human cavernosal contraction. J Androl. 2006 Sep-Oct;27(5):679-85. Epub 2006 May 25.


The effect of 5-HT on human cavernosal tissues, as well as those of doxazosin (shown previously to have 5-HT inhibitory action), ketanserin (5-HT (2A) receptor antagonist), NAN-190 (5-HT (1A) receptor antagonist), and SB 203186 (5-HT (4) receptor antagonist) on 5-HT-mediated effects, were assessed using the organ bath technique, including electrical field stimulation study (EFS).
3(0,0,0,3) 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
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.

In aggregates cultured with 1 nM estradiol for expression of the 5-HT4, -5, and -6 receptor (R), 5-HT promptly stimulated GH secretion with a dose dependency between 1 and 10 nM.
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.
1(0,0,0,1) Details
14656323 Paolucci E, Berretta N, Tozzi A, Bernardi G, Mercuri NB: Depression of mGluR-mediated IPSCs by 5-HT in dopamine neurons of the rat substantia nigra pars compacta. Eur J Neurosci. 2003 Nov;18(10):2743-50.

Similar results were obtained with alpha-methyl-5-hydroxytryptamine and 5-methoxytryptamine, but not with 5-carboxamidotryptamine or 1-(3-chlorophenyl) piperazine.
Our results demonstrate a powerful inhibition of the mGluR-IPSC by 5-HT in midbrain dopamine neurons, most probably through stimulation of 5-HT2A and 5-HT4 receptors.
1(0,0,0,1) Details
18295406 Qu CL, Huo FQ, Huang FS, Li YQ, Tang JS, Jia H: The role of 5-HT receptor subtypes in the ventrolateral orbital cortex of 5-HT-induced antinociception in the rat. Neuroscience. 2008 Mar 18;152(2):487-94. Epub 2007 Sep 21.

This study focused on the effects of 5-HT microinjection in the VLO of lightly anesthetized male rats on the radiant heat-evoked tail flick (TF) reflex, as well as the influence of 5-HT (1A), 5-HT (2), 5-HT (3), and 5-HT (4) receptor subtype antagonists on the effect of 5-HT.
Pretreatment with 5-HT receptor antagonists (1-(2-methoxyphenyl)-4-[4-(2-phthalimido) butyl] piperazine hydrobromide (NAN-190), cyproheptadine hydrochloride (CPT) and 1-methyl-N-(8-methyl-8-azabicyclo [3.2.3]-oct-3-yl)-1H-indazole-3-carboxami de maleate salt (LY-278,584)), specific for 5-HT (1A), 5-HT (2) and 5-HT (3) receptors, respectively, partially reversed the 5-HT-evoked inhibition.
1(0,0,0,1) Details
11167653 Testa R, Guarneri L, Angelico P, Velasco C, Poggesi E, Cilia A, Leonardi A: Effect of different 5-hydroxytryptamine receptor subtype antagonists on the micturition reflex in rats. BJU Int. 2001 Feb;87(3):256-64.


The tested antagonists of 5-HT2, 5-HT3, 5-HT4, and 5-HT6 serotoninergic subtypes were poorly active or inactive in the model.
1(0,0,0,1) 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
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