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Bemesetron
Systematic (IUPAC) name
[(1S,5R)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 3,5-dichlorobenzoate
Identifiers
CAS number 40796-97-2
ATC code none
PubChem 671690
ChemSpider 10498629
Chemical data
Formula C 15H17Cl2NO2  
Mol. mass 314.207 g/mol
SMILES eMolecules & PubChem
Synonyms Bemesetron
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes  ?

Bemesetron (MDL-72222) is a drug which acts as an antagonist at the 5HT3 receptor.[1] It has antiemetic effects comparable to metoclopramide,[2] 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.[3][4][5][6]

References

  1. ^ Shearman GT, Tolcsvai L (1987). "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 (Berl.) 92 (4): 520–3. PMID 3114804.  
  2. ^ Homesley HD, Hahne WF, McLees B, et al. (April 1993). "Randomized comparison of the antiemetic efficacy of a serotonin type 3 receptor antagonist (MDL 72,222) with a high-dose metoclopramide regimen". Am. J. Clin. Oncol. 16 (2): 175–9. PMID 8452114.  
  3. ^ McKinzie DL, McBride WJ, Murphy JM, Lumeng L, Li TK (October 2000). "Effects of MDL 72222, a serotonin3 antagonist, on operant responding for ethanol by alcohol-preferring P rats". Alcohol. Clin. Exp. Res. 24 (10): 1500–4. PMID 11045857. http://meta.wkhealth.com/pt/pt-core/template-journal/lwwgateway/media/landingpage.htm?issn=0145-6008&volume=24&issue=10&spage=1500.  
  4. ^ Kankaanpää A, Meririnne E, Seppälä T (February 2002). "5-HT3 receptor antagonist MDL 72222 attenuates cocaine- and mazindol-, but not methylphenidate-induced neurochemical and behavioral effects in the rat". Psychopharmacology (Berl.) 159 (4): 341–50. doi:10.1007/s00213-001-0939-410.1007/s00213-001-0939-4. PMID 11823886.  
  5. ^ Kos T, Popik P, Pietraszek M, et al. (May 2006). "Effect of 5-HT3 receptor antagonist MDL 72222 on behaviors induced by ketamine in rats and mice". Eur Neuropsychopharmacol 16 (4): 297–310. doi:10.1016/j.euroneuro.2005.10.001. PMID 16288851. http://linkinghub.elsevier.com/retrieve/pii/S0924-977X(05)00146-X.  
  6. ^ Yoo JH, Nam YS, Lee SY, Jang CG (January 2008). "Dopamine neurotransmission is involved in the attenuating effects of 5-HT3 receptor antagonist MDL 72222 on acute methamphetamine-induced locomotor hyperactivity in mice". Synapse 62 (1): 8–13. doi:10.1002/syn.2046110.1002/syn.20461. PMID 17948891.  
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