Bemesetron

drugbox
IUPAC_name = [(1S,5R)-8-methyl-8-azabicyclo [3.2.1] octan-3-yl] 3,5-dichlorobenzoate


width = 220
CAS_number = 40796-97-2
synonyms = Bemesetron
ATC_prefix =
ATC_suffix =
PubChem = 671690
DrugBank =
C = 15 | H = 17 | Cl = 2 | N = 1 | O = 2
molecular_weight = 314.207 g/mol
smiles = CN1 [C@H] 2CC [C@@H] 1CC(C2)OC(=O)C3=CC(=CC(=C3)Cl)Cl
bioavailability =
protein_bound =
metabolism =
elimination_half-life =
excretion =
pregnancy_AU =
pregnancy_US =
pregnancy_category=
legal_AU =
legal_CA =
legal_UK =
legal_US =
legal_status =
routes_of_administration =

Bemesetron (MDL-72222) is a drug which acts as an antagonist at the 5HT₃ receptor. [Shearman GT, Tolcsvai L. Effect of the selective 5-HT3 receptor antagonists ICS 205-930 and MDL 72222 on 5-HTP-induced head shaking and behavioral symptoms induced by 5-methoxy-N,N,dimethyltryptamine in rats: comparison with some other 5-HT receptor antagonists. "Psychopharmacology (Berlin)". 1987;92(4):520-3. PMID 3114804] It has antinauseant effects comparable to metoclopramide, [Homesley HD, Hahne WF, McLees B, Heck K, Barrett RJ, Lentz SS, Woodlief L, Lovelace JV. Randomized comparison of the antiemetic efficacy of a serotonin type 3 receptor antagonist (MDL 72,222) with a high-dose metoclopramide regimen. "American Journal of Clinical Oncology". 1993 Apr;16(2):175-9. PMID 8452114] however it is not used clinically, instead its main application is in scientific research studying the involvement of the 5HT₃ receptor in the actions of drugs of abuse. [McKinzie DL, McBride WJ, Murphy JM, Lumeng L, Li TK. Effects of MDL 72222, a serotonin3 antagonist, on operant responding for ethanol by alcohol-preferring P rats. "Alcohol, Clinical and Experimental Research". 2000 Oct;24(10):1500-4. PMID 11045857] [Kankaanpää A, Meririnne E, Seppälä T. 5-HT3 receptor antagonist MDL 72222 attenuates cocaine- and mazindol-, but not methylphenidate-induced neurochemical and behavioral effects in the rat. "Psychopharmacology (Berlin)". 2002 Feb;159(4):341-50. PMID 11823886] [Kos T, Popik P, Pietraszek M, Schäfer D, Danysz W, Dravolina O, Blokhina E, Galankin T, Bespalov AY. Effect of 5-HT3 receptor antagonist MDL 72222 on behaviors induced by ketamine in rats and mice. "European Neuropsychopharmacology". 2006 May;16(4):297-310. PMID 16288851] [Yoo JH, Nam YS, Lee SY, Jang CG. Dopamine neurotransmission is involved in the attenuating effects of 5-HT3 receptor antagonist MDL 72222 on acute methamphetamine-induced locomotor hyperactivity in mice. "Synapse". 2008 Jan;62(1):8-13. PMID 17948891]

References