Target family: 5-HT<sub>3</sub> receptors (type: lgic)
Target: 5-HT<sub>3</sub>A

Ligand: Zn2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Biphasic
Ligand approved: no
Median affinity:  -
Reference (Journal): An electrophysiological investigation of the properties of a murine recombinant 5-HT3 receptor stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: Zn2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Biphasic
Ligand approved: no
Median affinity:  -
Reference (Journal): Zn(2+) enhancement of the recombinant 5-HT(3) receptor is modulated by divalent cations.
Published in: Eur J Pharmacol

Ligand: vortioxetine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2013)
Primary target: yes
Median affinity: 8.430000305175781 pKi
Reference (Journal): Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
Published in: J Med Chem

Ligand: tubocurarine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1945)
Median affinity:  pKi
Reference (Journal): Interaction of D-tubocurarine analogs with the 5HT3 receptor.
Published in: Neuropharmacology

Ligand: tubocurarine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1945)
Median affinity: 4.8 pKi
Reference (Journal): Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: tubocurarine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1945)
Median affinity:  pKi
Reference (Journal): Allosteric interactions among agonists and antagonists at 5-hydroxytryptamine3 receptors.
Published in: J Neurochem

Ligand: tubocurarine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1945)
Median affinity: 4.8 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: tropisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig.
Published in: Mol Pharmacol

Ligand: tropisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: trichloroethanol (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Mutations of L293 in transmembrane two of the mouse 5-hydroxytryptamine3A receptor alter gating and alcohol modulatory actions.
Published in: Br J Pharmacol

Ligand: trichloroethanol (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): The interaction of trichloroethanol with murine recombinant 5-HT3 receptors.
Published in: Br J Pharmacol

Ligand: trichloroethanol (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Alcohols potentiate the function of 5-HT3 receptor-channels on NCB-20 neuroblastoma cells by favouring and stabilizing the open channel state.
Published in: J Physiol (Lond.)

Ligand: trichloroethanol (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Co-expression of the 5-HT(3B) subunit with the 5-HT(3A) receptor reduces alcohol sensitivity.
Published in: Brain Res Mol Brain Res

Ligand: trichloroethanol (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Arginine 246 of the pretransmembrane domain 1 region alters 2,2,2-trichloroethanol action in the 5-hydroxytryptamine3A receptor.
Published in: J Pharmacol Exp Ther

Ligand: TMB-8 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): A role for the Val291 residue within the transmembrane domain 2 in diltiazem- and TMB-8 [3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester]-mediated 5-hydroxytryptamine type 3A receptor regulations.
Published in: Biol Pharm Bull

Ligand: TMB-8 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 4.93 pIC50
Reference (Journal): Characterization of interaction of 3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester with Torpedo californica nicotinic acetylcholine receptor and 5-hydroxytryptamine3 receptor.
Published in: J Pharmacol Exp Ther

Ligand: TMB-8 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Characterization of interaction of 3,4,5-trimethoxybenzoic acid 8-(diethylamino)octyl ester with Torpedo californica nicotinic acetylcholine receptor and 5-hydroxytryptamine3 receptor.
Published in: J Pharmacol Exp Ther

Ligand: [3H]ramosetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.8 pKd
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: [3H]LY278584 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.51 pKd
Reference (Journal): Pharmacological and regional characterization of [3H]LY278584 binding sites in human brain.
Published in: J Neurochem

Ligand: [3H](S)-zacopride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pKd
Reference (Journal): Autoradiographic distribution of [3H]-(S)-zacopride-labelled 5-HT3 receptors in human brain.
Published in: J Neurol Sci

Ligand: [3H]meta-chlorophenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): Different efficacy of specific agonists at 5-HT3 receptor splice variants: the role of the extra six amino acid segment.
Published in: Br J Pharmacol

Ligand: [3H]granisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKd
Reference (Journal): Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: [3H]granisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKd
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: [3H]GR65630 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig.
Published in: Mol Pharmacol

Ligand: [3H]GR65630 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Evaluation of the pharmacological profile of ramosetron, a novel therapeutic agent for irritable bowel syndrome.
Published in: J Pharmacol Sci

Ligand: SR57227A (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pEC50
Reference (Journal): 5-HT3-like receptors in the rat medial prefrontal cortex: further pharmacological characterization.
Published in: Brain Res

Ligand: ricasetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: ramosetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10 pKi
Reference (Journal): Evaluation of the pharmacological profile of ramosetron, a novel therapeutic agent for irritable bowel syndrome.
Published in: J Pharmacol Sci

Ligand: quipazine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.5 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: picrotoxinin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 4.96 pIC50
Reference (Journal): Binding sites for bilobalide, diltiazem, ginkgolide, and picrotoxinin at the 5-HT3 receptor.
Published in: Mol Pharmacol

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): The 5-HT3B subunit confers reduced sensitivity to picrotoxin when co-expressed with the 5-HT3A receptor.
Published in: Brain Res Mol Brain Res

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): The GABA(A) receptor antagonist picrotoxin inhibits 5-hydroxytryptamine type 3A receptors.
Published in: Neuropharmacology

Ligand: palonosetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2003), EMA (2009)
Primary target: yes
Median affinity: 10.489999771118164 pKi
Reference (Journal): Computational analysis of ligand recognition sites of homo- and heteropentameric 5-HT3 receptors.
Published in: Eur J Med Chem

Ligand: ondansetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1991)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: ondansetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1991)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Molecular cloning of human 5-hydroxytryptamine3 receptor: heterogeneity in distribution and function among species.
Published in: Mol Pharmacol

Ligand: ondansetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1991)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: Mg2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  -
Reference (Journal): The role of the agonist binding site in Ca(2+) inhibition of the recombinant 5-HT(3A) receptor.
Published in: Eur J Pharmacol

Ligand: Mg2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  -
Reference (Journal): Ion permeation properties of a cloned human 5-HT3 receptor transiently expressed in HEK 293 cells.
Published in: Amino Acids

Ligand: Mg2+ (Inorganic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity:  -
Reference (Journal): An electrophysiological investigation of the properties of a murine recombinant 5-HT3 receptor stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: metoclopramide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1979)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
Published in: Br J Pharmacol

Ligand: metoclopramide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1979)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: (S)-zacopride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: (R)-zacopride (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig.
Published in: Mol Pharmacol

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Cloning and functional expression of a human 5-hydroxytryptamine type 3AS receptor subunit.
Published in: Mol Pharmacol

Ligand: meta-chlorphenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular cloning, functional expression, and pharmacological characterization of 5-hydroxytryptamine3 receptor cDNA and its splice variants from guinea pig.
Published in: Mol Pharmacol