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
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 :

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