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

Ligand: tubocurarine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1945)
Median affinity: 4.5 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

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: [3H]granisetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.8 pKd
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: quipazine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: 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: picrotoxinin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 4.2 pIC50
Reference (Journal): Ginkgolide B and bilobalide block the pore of the 5-HT(3) receptor at a location that overlaps the picrotoxin binding site.
Published in: Neuropharmacology

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 2.9 pIC50
Reference (Journal): Molecular determinants of picrotoxin inhibition of 5-hydroxytryptamine type 3 receptors.
Published in: J Pharmacol Exp Ther

Ligand: picrotoxin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 2.9 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: ondansetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1991)
Primary target: yes
Median affinity: 7.800000190734863 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: metoclopramide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1979)
Primary target: yes
Median affinity: 5.699999809265137 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
Median affinity: 8.8 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: 7.7 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: 7 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: 5.7 pEC50
Reference (Journal): The 5-HT3B subunit is a major determinant of serotonin-receptor function.
Published in: Nature

Ligand: ginkgolide B (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 2.41 pIC50
Reference (Journal): Ginkgolide B and bilobalide block the pore of the 5-HT(3) receptor at a location that overlaps the picrotoxin binding site.
Published in: Neuropharmacology

Ligand: CSTI-300 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): CSTI-300 (SMP-100); a Novel 5-HT<sub>3</sub> Receptor Partial Agonist with Potential to Treat Patients with Irritable Bowel Syndrome or Carcinoid Syndrome.
Published in: J Pharmacol Exp Ther

Ligand: cocaine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
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: bilobalide (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 2.51 pIC50
Reference (Journal): Ginkgolide B and bilobalide block the pore of the 5-HT(3) receptor at a location that overlaps the picrotoxin binding site.
Published in: Neuropharmacology

Ligand: azasetron (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 8.4 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The pharmacological and functional characteristics of the serotonin 5-HT(3A) receptor are specifically modified by a 5-HT(3B) receptor subunit.
Published in: J Biol Chem

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Probing the role of a conserved M1 proline residue in 5-hydroxytryptamine(3) receptor gating.
Published in: Mol Pharmacol

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The 5-HT3B subunit is a major determinant of serotonin-receptor function.
Published in: Nature

Ligand: 5-hydroxytryptamine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): General anesthetic-induced channel gating enhancement of 5-hydroxytryptamine type 3 receptors depends on receptor subunit composition.
Published in: J Pharmacol Exp Ther

Ligand: 2-methyl-5-HT (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.9 pEC50
Reference (Journal): The 5-HT3B subunit is a major determinant of serotonin-receptor function.
Published in: Nature

Ligand: 1-phenylbiguanide (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.9 pKi
Reference (Journal): Pharmacological comparison of human homomeric 5-HT3A receptors versus heteromeric 5-HT3A/3B receptors.
Published in: Neuropharmacology