Agonists for serotonin receptor 5-HT3 subtype
 
 
 
Agonist Subtype Other name(s) Affinity Structure

5-HT

non specific

5-Hydroxytryptamine, Serotonin;
Indol-5-ol3-(b-Aminoethyl)-5-hydroxyindole3-(2-
aminoethyl)indol-5-ol 5-HTA; 
5-Hydroxy-3-(b-aminoethyl)indole;
Antemovis; 
Enteramin; 
Substance DS; ThrombocytinThrombotonin
 

EC50 = 2.2m M

(N1E-115 cells)


2-Me-5-HT  5-HT3 2-methyl-5-HT;
2-Methyl-5-hydroxytryptamine;
2-Methylserotonin;
 
IC50 = 0.04-0.8 m M

EC50 = 9.9m M

5-CT 5-HT2A
novel?
5-Carboxamidotryptamine
 
 
 
 
 
Benzoxazole 5-HT3
partial agonist/
antagonist
1-Oxa-3-aza-1H-indene;
1-Oxa-3-azaindene
 
mCPBG 5-HT3 m-Chlorophenylbiguanide ;
Biguanide
EC50 = 0.76m M
Isatin 5-HT3 Indole-2,3-dione (8CI);
2,3-Dihydro-1H-indole-2,3-dione;
2,3-Diketoindoline;
2,3-Dioxo-2,3-dihydroindole;
2,3-Dioxoindoline; 2,3-Indolinedione;
Isatic acid lactam; Isatinic acid anhydride;
o-Aminobenzoylformic anhydride;
Pseudoisatin
antagonist for APN (atrial natriuretic peptide receptor)
Neostigmine AChE antagonist Ammonium, (m-hydroxyphenyl)-trimethyl-, dimethylcarbamate (ester) (8CI);
Eustigmin;
Prostigmin; Prostigmine; 
Vagostigmine;
m-rimethylammonium-phenyl-dimethylcarbamate
acetylcholine esterase inhibition potentiates 5-HT3 agonist activity
Phenyl-biguanide (PBG) 5-HT3 Biguanide-1-phenyl- (6CI, 7CI, 8CI);
1-Phenylbiguanide;
N-Phenyl-N'-guanylguanidine;
N-Phenylbiguanide; 
N1-Phenylbiguanide
EC50 = 22m M
Piperazine derivatives (heterocyclic) 5-HT3 1,4-Diazacyclohexane;
1,4-Piperazine; Antiren; Diethylenediamine;
Dispermine; Eraverm; Hexahydropyrazine;
Lumbrical; Piperazidine; Pipersol;
Pyrazine hexahydride; Uvilon; Vermex; Worm-A-Ton; Wurmirazin
 
Quipazine 5-HT3 Quinoline, 2-(1-piperazinyl) KD = 0.62nM
S 21007 5-HT3

partial

Pyrrolo[1,2-a]thieno[3,2-e]pyrazine, 5-[4-(phenylm ethyl)-1-piperazinyl]- (9CI)  EC50 = 27m M 

IC50 = 2.8nM

SR 57227A 5-HT3 CM 57277 EC50 = 0.2-11m M