Proteins > 5-hydroxytryptamine receptor 3A
Page last updated: 2024-08-07 16:41:50
5-hydroxytryptamine receptor 3A
A 5-hydroxytryptamine receptor 3A that is encoded in the genome of human. [PRO:DNx, UniProtKB:P46098]
Synonyms
5-HT3-A;
5-HT3A;
5-hydroxytryptamine receptor 3;
5-HT-3;
5-HT3R;
Serotonin receptor 3A;
Serotonin-gated ion channel receptor
Research
Bioassay Publications (86)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (1.16) | 18.7374 |
| 1990's | 14 (16.28) | 18.2507 |
| 2000's | 34 (39.53) | 29.6817 |
| 2010's | 32 (37.21) | 24.3611 |
| 2020's | 5 (5.81) | 2.80 |
Compounds (102)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 1-(1-naphthyl)piperazine | Homo sapiens (human) | Ki | 0.1750 | 1 | 2 |
| 1-(2-methoxyphenyl)piperazine | Homo sapiens (human) | Ki | 2.5000 | 1 | 2 |
| 1-(3-chlorophenyl)biguanide | Homo sapiens (human) | Ki | 0.0174 | 4 | 5 |
| 1-(3-chlorophenyl)piperazine | Homo sapiens (human) | Ki | 0.0620 | 1 | 2 |
| 2-methyl-5-ht | Homo sapiens (human) | Ki | 1.2000 | 1 | 1 |
| alosetron | Homo sapiens (human) | Ki | 0.0005 | 3 | 3 |
| buspirone | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| cgs 12066 | Homo sapiens (human) | IC50 | 1.3183 | 1 | 1 |
| eucalyptol | Homo sapiens (human) | IC50 | 257.0400 | 1 | 1 |
| cisapride | Homo sapiens (human) | Ki | 1.3808 | 3 | 3 |
| n(6),n(6)-dimethyladenine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| granisetron | Homo sapiens (human) | Ki | 0.0095 | 5 | 6 |
| mianserin | Homo sapiens (human) | IC50 | 1.4125 | 2 | 2 |
| mirtazapine | Homo sapiens (human) | Ki | 2.9000 | 1 | 1 |
| 1-(3-trifluoromethylphenyl)piperazine | Homo sapiens (human) | Ki | 1.3900 | 1 | 2 |
| ondansetron | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
| ondansetron | Homo sapiens (human) | Ki | 0.0100 | 6 | 7 |
| phenyl biguanide | Homo sapiens (human) | Ki | 1.2000 | 3 | 4 |
| quipazine | Homo sapiens (human) | IC50 | 0.0004 | 1 | 1 |
| quipazine | Homo sapiens (human) | Ki | 0.0027 | 3 | 5 |
| 6-nitroquipazine | Homo sapiens (human) | Ki | 0.0580 | 1 | 1 |
| n-methylquipazine | Homo sapiens (human) | IC50 | 0.0047 | 1 | 1 |
| n-methylquipazine | Homo sapiens (human) | Ki | 0.0022 | 2 | 3 |
| rizatriptan | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sdz 205-557 | Homo sapiens (human) | Ki | 0.1259 | 1 | 1 |
| sumatriptan | Homo sapiens (human) | IC50 | 3.3385 | 4 | 6 |
| 6-methylthiopurine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| linalool | Homo sapiens (human) | IC50 | 141.2540 | 1 | 1 |
| phenylpiperazine | Homo sapiens (human) | Ki | 3.0000 | 1 | 2 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| amanozine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| phenylguanidine | Homo sapiens (human) | Ki | 2.3400 | 2 | 3 |
| 4-chlorophenylbiguanide | Homo sapiens (human) | Ki | 0.2033 | 2 | 3 |
| aripiprazole | Homo sapiens (human) | Ki | 0.5012 | 1 | 1 |
| ziprasidone | Homo sapiens (human) | Ki | 0.3981 | 1 | 1 |
| lerisetron | Homo sapiens (human) | Ki | 0.0004 | 1 | 1 |
| 4-phenylpiperidine | Homo sapiens (human) | Ki | 10.0000 | 1 | 2 |
| nicotine | Homo sapiens (human) | Ki | 71.0000 | 1 | 2 |
| 1-(4-chlorophenyl)piperazine | Homo sapiens (human) | Ki | 2.1600 | 1 | 2 |
| gr 127935 | Homo sapiens (human) | Ki | 6.3096 | 1 | 1 |
| ramosetron | Homo sapiens (human) | Ki | 0.0001 | 1 | 1 |
| zacopride | Homo sapiens (human) | Ki | 0.0005 | 2 | 3 |
| gr 113808 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| pramipexole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sb 204070a | Homo sapiens (human) | Ki | 0.2031 | 3 | 3 |
| sr 57227a | Homo sapiens (human) | Ki | 0.1030 | 1 | 1 |
| sc 53116 | Homo sapiens (human) | Ki | 0.1520 | 2 | 2 |
| harmalan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| piboserod | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| rs 23597-190 | Homo sapiens (human) | Ki | 1.9953 | 1 | 1 |
| ngd 94-1 | Homo sapiens (human) | Ki | 0.7500 | 1 | 1 |
| 1-(4-methoxyphenyl)piperazine | Homo sapiens (human) | Ki | 1.6400 | 1 | 2 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| tropisetron | Homo sapiens (human) | Ki | 0.0082 | 6 | 7 |
| bemesetron | Homo sapiens (human) | IC50 | 0.0928 | 9 | 9 |
| bemesetron | Homo sapiens (human) | Ki | 0.0055 | 5 | 5 |
| 4-(benzylsulfanyl)thieno[2,3-d]pyrimidine | Homo sapiens (human) | IC50 | 9.0000 | 1 | 1 |
| 2-(4-chlorophenyl)guanidine | Homo sapiens (human) | Ki | 0.3220 | 2 | 3 |
| norcisapride | Homo sapiens (human) | IC50 | 1.6000 | 1 | 1 |
| prucalopride | Homo sapiens (human) | Ki | 3.9811 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 6-methylpurine | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| l 745870 | Homo sapiens (human) | Ki | 9.9000 | 1 | 1 |
| naltrexone | Homo sapiens (human) | Ki | 0.0600 | 1 | 1 |
| batimastat | Homo sapiens (human) | IC50 | 0.0250 | 1 | 1 |
| palonosetron | Homo sapiens (human) | IC50 | 0.0030 | 10 | 10 |
| palonosetron | Homo sapiens (human) | Ki | 0.0000 | 1 | 1 |
| 1-(3-(5-(1,2,4-triazol-4-yl)-1h-indol-3-yl)propyl)-4-(2-(3-fluorophenyl)ethyl)piperazine | Homo sapiens (human) | IC50 | 9.2500 | 2 | 4 |
| sb 269970 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sarizotan | Homo sapiens (human) | IC50 | 0.0060 | 1 | 1 |
| 2-ethyl-5-methoxy-n,n-dimethyltryptamine | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
| azd 0328 | Homo sapiens (human) | Ki | 0.0120 | 1 | 1 |
| pnu-282987 | Homo sapiens (human) | Ki | 2.3773 | 3 | 3 |
| ssr180711 | Homo sapiens (human) | IC50 | 3.1600 | 1 | 1 |
| s 21007 | Homo sapiens (human) | IC50 | 0.0014 | 3 | 3 |
| s 21007 | Homo sapiens (human) | Ki | 0.0010 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| vortioxetine | Homo sapiens (human) | Ki | 0.0037 | 1 | 1 |
| 5-chloro-2-methyl-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1h-indole | Homo sapiens (human) | IC50 | 0.0340 | 1 | 1 |
| m-chlorophenylguanidine | Homo sapiens (human) | Ki | 0.0335 | 5 | 6 |
| fauc 113 | Homo sapiens (human) | Ki | 12.0000 | 1 | 1 |
| barettin | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 5-hydroxy-2-(2-phenylethyl)chromone | Homo sapiens (human) | Ki | 2.5119 | 1 | 1 |
| af 353 | Homo sapiens (human) | Ki | 100,000.0000 | 1 | 1 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| vuf10166 | Homo sapiens (human) | Ki | 0.0110 | 2 | 2 |
| cep 26401 | Homo sapiens (human) | Ki | 0.0020 | 1 | 1 |
| pf 3246799 | Homo sapiens (human) | IC50 | 2.3000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| evp-6124 | Homo sapiens (human) | IC50 | 0.2990 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| a-1155463 | Homo sapiens (human) | Ki | 1.1189 | 2 | 0 |
| clozapine | Homo sapiens (human) | Ki | 0.3348 | 3 | 3 |
| olanzapine | Homo sapiens (human) | Ki | 0.1995 | 1 | 1 |
| tegaserod | Homo sapiens (human) | Ki | 6.2559 | 2 | 2 |
| methylaplysinopsin | Homo sapiens (human) | Ki | 1.5110 | 1 | 1 |
| aplysinopsin | Homo sapiens (human) | Ki | 3.0290 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| granisetron | Homo sapiens (human) | Kb | 0.0129 | 1 | 1 |
| ondansetron | Homo sapiens (human) | Kb | 0.0194 | 1 | 1 |
| metergoline | Homo sapiens (human) | Activity | 10.0000 | 1 | 1 |
| tropisetron | Homo sapiens (human) | Kb | 0.0093 | 1 | 1 |
Progress in the discovery of small molecule modulators of the Cys-loop superfamily receptors.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 27, Issue:15, 2017
Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG).Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
Electrostatic potential surfaces of 5-HT(3)R agonists suggest accessory cation-pi site adjacent to agonist binding domain.Bioorganic & medicinal chemistry letters, , Oct-07, Volume: 12, Issue:19, 2002
The binding of arylguanidines at 5-HT(3) serotonin receptors: a structure-affinity investigation.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
The discovery of diazepinone-based 5-HT3 receptor partial agonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 24, Issue:11, 2014
Novel serotonin type 3 receptor partial agonists for the potential treatment of irritable bowel syndrome.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 20, Issue:22, 2010
Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 23, Issue:14, 2013
5-HT4 receptor ligands: applications and new prospects.Journal of medicinal chemistry, , Jan-30, Volume: 46, Issue:3, 2003
Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
High-affinity fluorescent ligands for the 5-HT(3) receptor.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
Toward biophysical probes for the 5-HT3 receptor: structure-activity relationship study of granisetron derivatives.Journal of medicinal chemistry, , Mar-11, Volume: 53, Issue:5, 2010
Computational analysis of ligand recognition sites of homo- and heteropentameric 5-HT3 receptors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Phenylimidazolidin-2-one derivatives as selective 5-HT3 receptor antagonists and refinement of the pharmacophore model for 5-HT3 receptor binding.Journal of medicinal chemistry, , Oct-10, Volume: 40, Issue:21, 1997
5-HT3 receptor antagonists. 3. Quinoline derivatives which may be effective in the therapy of irritable bowel syndrome.Journal of medicinal chemistry, , Oct-29, Volume: 36, Issue:22, 1993
Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.Journal of medicinal chemistry, , Volume: 33, Issue:6, 1990
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 2.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
Synthesis and structure-activity relationship of 2-(aminoalkyl)-2,3,3a,8-tetrahydrodibenzo[c,f]isoxazolo[2,3-a]azepine derivatives: a novel series of 5-HT(2A/2C) receptor antagonists. Part 1.Bioorganic & medicinal chemistry letters, , Jan-21, Volume: 12, Issue:2, 2002
Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.Journal of medicinal chemistry, , May-12, Volume: 54, Issue:9, 2011
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 20, Issue:22, 2010
The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
Phenylimidazolidin-2-one derivatives as selective 5-HT3 receptor antagonists and refinement of the pharmacophore model for 5-HT3 receptor binding.Journal of medicinal chemistry, , Oct-10, Volume: 40, Issue:21, 1997
5-HT3 receptor antagonists. 3. Quinoline derivatives which may be effective in the therapy of irritable bowel syndrome.Journal of medicinal chemistry, , Oct-29, Volume: 36, Issue:22, 1993
An initial three-component pharmacophore for specific serotonin-3 receptor ligands.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.Journal of medicinal chemistry, , Volume: 33, Issue:6, 1990
Electrostatic potential surfaces of 5-HT(3)R agonists suggest accessory cation-pi site adjacent to agonist binding domain.Bioorganic & medicinal chemistry letters, , Oct-07, Volume: 12, Issue:19, 2002
The binding of arylguanidines at 5-HT(3) serotonin receptors: a structure-affinity investigation.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor.Journal of medicinal chemistry, , Sep-20, Volume: 50, Issue:19, 2007
Electrostatic potential surfaces of 5-HT(3)R agonists suggest accessory cation-pi site adjacent to agonist binding domain.Bioorganic & medicinal chemistry letters, , Oct-07, Volume: 12, Issue:19, 2002
Pyrroloquinoxaline derivatives as high-affinity and selective 5-HT(3) receptor agonists: synthesis, further structure-activity relationships, and biological studies.Journal of medicinal chemistry, , Oct-21, Volume: 42, Issue:21, 1999
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Design, synthesis, and structure-activity relationships of highly potent 5-HT₃ receptor ligands.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Selective, orally active 5-HT1D receptor agonists as potential antimigraine agents.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Synthesis and serotonergic activity of N,N-dimethyl-2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethylamine and analogues: potent agonists for 5-HT1D receptors.Journal of medicinal chemistry, , May-12, Volume: 38, Issue:10, 1995
The binding of arylguanidines at 5-HT(3) serotonin receptors: a structure-affinity investigation.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
The binding of arylguanidines at 5-HT(3) serotonin receptors: a structure-affinity investigation.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
An initial three-component pharmacophore for specific serotonin-3 receptor ligands.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
(1-Butyl-4-piperidinyl)methyl 8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride: a highly potent and selective 5-HT4 receptor antagonist derived from metoclopramide.Journal of medicinal chemistry, , Dec-10, Volume: 36, Issue:25, 1993
Bridgehead-methyl analog of SC-53116 as a 5-HT4 agonist.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
5-HT4 receptor ligands: applications and new prospects.Journal of medicinal chemistry, , Jan-30, Volume: 46, Issue:3, 2003
Return of DJournal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Discovery and development of α7 nicotinic acetylcholine receptor modulators.Journal of medicinal chemistry, , Dec-08, Volume: 54, Issue:23, 2011
Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.Bioorganic & medicinal chemistry letters, , Feb-12, Volume: 11, Issue:3, 2001
New benzocycloalkylpiperazines, potent and selective 5-HT1A receptor ligands.Journal of medicinal chemistry, , Mar-14, Volume: 40, Issue:6, 1997
Phenylimidazolidin-2-one derivatives as selective 5-HT3 receptor antagonists and refinement of the pharmacophore model for 5-HT3 receptor binding.Journal of medicinal chemistry, , Oct-10, Volume: 40, Issue:21, 1997
An initial three-component pharmacophore for specific serotonin-3 receptor ligands.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Thiazole as a carbonyl bioisostere. A novel class of highly potent and selective 5-HT3 receptor antagonists.Journal of medicinal chemistry, , Volume: 33, Issue:10, 1990
Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.Journal of medicinal chemistry, , Volume: 33, Issue:6, 1990
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CHBioorganic & medicinal chemistry, , 01-15, Volume: 25, Issue:2, 2017
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.Bioorganic & medicinal chemistry, , Apr-15, Volume: 24, Issue:8, 2016
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.Bioorganic & medicinal chemistry, , May-15, Volume: 21, Issue:10, 2013
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Quinazolindione derivatives as potent 5-HT3A receptor antagonists.Bioorganic & medicinal chemistry, , Jul-01, Volume: 17, Issue:13, 2009
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
High affinity ligands for the alpha7 nicotinic receptor that show no cross-reactivity with the 5-HT3 receptor.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.Journal of medicinal chemistry, , Volume: 33, Issue:6, 1990
The binding of arylguanidines at 5-HT(3) serotonin receptors: a structure-affinity investigation.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
[no title available]Journal of medicinal chemistry, , 09-23, Volume: 64, Issue:18, 2021
Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Computational analysis of ligand recognition sites of homo- and heteropentameric 5-HT3 receptors.European journal of medicinal chemistry, , Volume: 45, Issue:11, 2010
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationshJournal of medicinal chemistry, , Jul-13, Volume: 49, Issue:14, 2006
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
First tricyclic oximino derivatives as 5-HT3 ligands.Bioorganic & medicinal chemistry letters, , Feb-26, Volume: 11, Issue:4, 2001
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.Journal of medicinal chemistry, , Jun-06, Volume: 40, Issue:12, 1997
2-Amino-6-chloro-3,4-dihydroquinazoline: A novel 5-HT3 receptor antagonist with antidepressant character.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 23, Issue:21, 2013
Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG).Bioorganic & medicinal chemistry letters, , Mar-24, Volume: 13, Issue:6, 2003
Electrostatic potential surfaces of 5-HT(3)R agonists suggest accessory cation-pi site adjacent to agonist binding domain.Bioorganic & medicinal chemistry letters, , Oct-07, Volume: 12, Issue:19, 2002
The binding of arylguanidines at 5-HT(3) serotonin receptors: a structure-affinity investigation.Bioorganic & medicinal chemistry letters, , Jun-18, Volume: 11, Issue:12, 2001
Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.Journal of medicinal chemistry, , Oct-18, Volume: 50, Issue:21, 2007
Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.Bioorganic & medicinal chemistry letters, , Jan-04, Volume: 9, Issue:1, 1999
Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 23, Issue:14, 2013
Novel antagonists of serotonin-4 receptors: synthesis and biological evaluation of pyrrolothienopyrazines.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Enables
This protein enables 7 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| serotonin-gated monoatomic cation channel activity | molecular function | Enables the transmembrane transfer of a cation by a channel that opens when serotonin has been bound by the channel complex or one of its constituent parts. [GOC:mtg_transport, PMID:12867984] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| serotonin binding | molecular function | Binding to serotonin (5-hydroxytryptamine), a monoamine neurotransmitter occurring in the peripheral and central nervous systems, also having hormonal properties. [GOC:ai] |
| ligand-gated monoatomic ion channel activity involved in regulation of presynaptic membrane potential | molecular function | Any ligand-gated ion channel activity, occurring in the presynaptic membrane, that is involved in regulation of presynaptic membrane potential. [GOC:dos, PMID:15145529, PMID:19558451] |
| transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potential | molecular function | Any transmitter-gated ion channel activity that is involved in regulation of postsynaptic membrane potential. [GO_REF:0000061, GOC:TermGenie, PMID:20200227] |
| excitatory extracellular ligand-gated monoatomic ion channel activity | molecular function | Enables the transmembrane transfer of an ion by a channel that opens when a specific extracellular ligand has been bound by the channel complex or one of its constituent parts, where channel opening contributes to an increase in membrane potential. [GOC:mah, ISBN:0323037070] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cleavage furrow | cellular component | The cleavage furrow is a plasma membrane invagination at the cell division site. The cleavage furrow begins as a shallow groove and eventually deepens to divide the cytoplasm. [GOC:vw, ISBN:0805319409] |
| postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| neuron projection | cellular component | A prolongation or process extending from a nerve cell, e.g. an axon or dendrite. [GOC:jl, http://www.cogsci.princeton.edu/~wn/] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| serotonin-activated cation-selective channel complex | cellular component | A protein complex which is capable of serotonin-activated cation-selective channel activity. Mainly found in pre- and postsynaptic membranes of the brain and gastrointestinal tract. Depending on its location it transports Ca2+, Mg2+, Na+ or K+. It is always a pentamer, containing at least the 5HT3A subunit forming 5HT3A homopentamers or 5HT3A/B heteropentamers. In human, 5HT3A/C, A/D and A/E heteropentamers also exist. [GO_REF:0000088, GOC:bhm, GOC:TermGenie, PMID:16116092] |
| transmembrane transporter complex | cellular component | A transmembrane protein complex which enables the transfer of a substance from one side of a membrane to the other. [GOC:bhm, GOC:TermGenie, PMID:18024586] |
Involved In
This protein is involved in 7 target(s):
| Target | Category | Definition |
|---|
| serotonin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a serotonin receptor binding to one of its physiological ligands. [GOC:mah] |
| monoatomic ion transmembrane transport | biological process | A process in which a monoatomic ion is transported across a membrane. Monatomic ions (also called simple ions) are ions consisting of exactly one atom. [GOC:mah] |
| excitatory postsynaptic potential | biological process | A process that leads to a temporary increase in postsynaptic potential due to the flow of positively charged ions into the postsynaptic cell. The flow of ions that causes an EPSP is an excitatory postsynaptic current (EPSC) and makes it easier for the neuron to fire an action potential. [GOC:dph, GOC:ef] |
| inorganic cation transmembrane transport | biological process | A process in which an inorganic cation is transported from one side of a membrane to the other by means of some agent such as a transporter or pore. [GOC:mah] |
| regulation of presynaptic membrane potential | biological process | Any process that modulates the potential difference across a presynaptic membrane. [GOC:dph, GOC:ef] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |
| regulation of membrane potential | biological process | Any process that modulates the establishment or extent of a membrane potential, the electric potential existing across any membrane arising from charges in the membrane itself and from the charges present in the media on either side of the membrane. [GOC:jl, GOC:mtg_cardio, GOC:tb, ISBN:0198506732] |