Proteins > 5-hydroxytryptamine receptor 3C
Page last updated: 2024-08-07 17:20:22
5-hydroxytryptamine receptor 3C
A 5-hydroxytryptamine receptor 3C that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q8WXA8]
Synonyms
5-HT3-C;
5-HT3C;
Serotonin receptor 3C
Research
Bioassay Publications (32)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 1 (3.13) | 18.7374 |
1990's | 12 (37.50) | 18.2507 |
2000's | 18 (56.25) | 29.6817 |
2010's | 0 (0.00) | 24.3611 |
2020's | 1 (3.13) | 2.80 |
Compounds (52)
Drugs with Inhibition Measurements
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 |
tropisetron | Homo sapiens (human) | Kb | 0.0093 | 1 | 1 |
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 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
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
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
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
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 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
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
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
Positron Emission Tomography (PET) Imaging Tracers for Serotonin Receptors.Journal of medicinal chemistry, , 08-25, Volume: 65, Issue:16, 2022
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
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
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
Enables
This protein enables 4 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] |
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] |
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] |
Located In
This protein is located in 2 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] |
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] |
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/] |
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] |
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 6 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 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] |
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] |