5-HT3 Receptors

Serotonin 5-HT3 receptors, are ligand-gated ion channels of the Cys-loop family. The receptor consists of four transmembrane domains that form an intrinsic cation-selective channel. So far five human 5-HT3 receptor subtypes have been identified (5-HT3A-E).

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
0440 m-Chlorophenylbiguanide hydrochloride
Potent and selective 5-HT3 agonist
0558 2-Methyl-5-hydroxytryptamine hydrochloride
5-HT3 agonist/potent 5-HT6 ligand
0566 N-Methylquipazine dimaleate
5-HT3 agonist
0969 1-Phenylbiguanide hydrochloride
5-HT3 agonist
0629 Quipazine dimaleate
5-HT3 agonist
0988 RS 56812 hydrochloride
5-HT3 partial agonist
3547 Serotonin hydrochloride
Endogenous 5-HT receptor agonist
1205 SR 57227 hydrochloride
Potent, selective 5-HT3 agonist

Antagonists

Cat No Product Name / Activity
0666 3-AQC
5-HT3 antagonist
2759 B-HT 920
5-HT3 antagonist. Also D2 and α2 agonist
5629 Dolasetron mesylate
Potent and selective 5-HT3 antagonist
2903 Granisetron hydrochloride
5-HT3 antagonist
0640 MDL 72222
5-HT3 antagonist
2018 Mirtazapine
Potent 5-HT3 antagonist. Also 5-HT2, H1 and α2-antagonist. Antidepressant
2844 Mosapride citrate
5-HT3 antagonist and 5-HT4 agonist
2891 Ondansetron hydrochloride
Selective 5-HT3 antagonist
2037 SDZ 205-557 hydrochloride
5-HT3/5-HT4 receptor antagonist
0641 Tropanyl-3,5-dimethylbenzoate
5-HT3 antagonist
2459 Tropisetron hydrochloride
Potent 5-HT3 receptor antagonist; also partial agonist of α7 nAChR
4532 VUF 10166
High affinity 5-HT3 receptor antagonist
0380 Y-25130 hydrochloride
Potent, selective 5-HT3 antagonist
1795 Zacopride hydrochloride
Highly potent 5-HT3 receptor antagonist. Also 5-HT4 agonist

Modulators

Cat No Product Name / Activity
4700 PU 02
Negative allosteric modulator of 5-HT3

Ligands

Cat No Product Name / Activity
1015 RS 16566 dihydrochloride
5-HT3 ligand. Also shows affinity for zacopride binding site

Other

Cat No Product Name / Activity
3306 8-(3-Chlorostyryl)caffeine
MAO-B inhibitor. Also A2A antagonist
0357 N-Acetyltryptamine
Serotonin N-acetyltransferase substrate
2813 D-Amphetamine sulfate
Induces 5-HT, dopamine and noradrenalin release
0767 Bifemelane hydrochloride
MAO-A and MAO-B inhibitor
0938 p-Chlorophenylalanine
Tryptophan hydroxylase inhibitor
1095 (R)-(-)-Deprenyl hydrochloride
MAO-B inhibitor
2695 Dexfenfluramine hydrochloride
5-HT re-uptake inhibitor. Also stimulates 5-HT release
0474 Dihydroergocristine mesylate
5-HT antagonist. Also partial agonist at adrenergic and dopaminergic receptors
0475 Dihydroergotamine mesylate
5-HT antagonist. Also partial agonist at adrenergic and dopaminergic D2 receptors
1132 Harmane
MAO-A and MAO-B inhibitor
2460 Lazabemide hydrochloride
Selective MAO-B inhibitor
4395 Moclobemide
Reversible MAO-A inhibitor
0610 Parthenolide
5-HT release inhibitor
3045 Pemoline
CNS stimulant, indirect monoamine agonist
0724 Pirlindole mesylate
MAO-A inhibitor
4308 Rasagiline mesylate
Selective, irreversible MAO-B inhibitor
0723 Tetrindole mesylate
MAO-A inhibitor

Serotonin 5-HT3 receptors, are ligand-gated ion channels of the Cys-loop family. The receptor consists of 4-transmembrane domains that form an intrinsic cation-selective channel. So far five human 5-HT3 receptor subtypes have been identified (5-HT3A-E).

The 5-HT3B-E subtypes do not form functional homo-oligomeric complexes like the 5-HT3A subtypes, but co-assemble with 5-HT3A to influence its functional expression.

External sources of pharmacological information for 5-HT3 Receptors :

Literature for 5-HT3 Receptors

5-HT Receptors

5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

5-HT3 Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
5-HT3A Human HTR3A NM_000869 P46098
Mouse Htr3a NM_013561 P23979
Rat Htr3a NM_024394 P35563
5-HT3B Human HTR3B NM_006028 O95264
Mouse Htr3b NM_020274 Q9JHJ5
Rat Htr3b NM_022189 Q9JJ16
5-HT3C Human HTR3C NM_130770 Q8WXA8
5-HT3D Human HTR3D NM_182537 Q70Z44
5-HT3E Human HTR3E NM_182589 A5X5Y0