贝美司琼

化合物

贝美司琼INN:bemesetron;开发代号:MDL-72222)是一种用作5-HT3受体拮抗剂的药物。[1]它具有与甲氧氯普胺相当的止吐作用,[2]然而它不用于临床,其主要应用是在科学研究中,研究5-HT3受体与滥用药物作用的关系。[3][4][5][6]

贝美司琼
臨床資料
ATC碼
  • 未分配
识别信息
  • [(1S,5R)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl] 3,5-dichlorobenzoate
CAS号40796-97-2  checkY
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard英语CompTox Chemicals Dashboard (EPA)
ECHA InfoCard100.164.757 編輯維基數據鏈接
化学信息
化学式C15H17Cl2NO2
摩尔质量314.21 g·mol−1
3D模型(JSmol英语JSmol
  • CN3[C@@H]1CC[C@H]3C[C@H](C1)OC(=O)c2cc(Cl)cc(Cl)c2
  • InChI=1S/C15H17Cl2NO2/c1-18-12-2-3-13(18)8-14(7-12)20-15(19)9-4-10(16)6-11(17)5-9/h4-6,12-14H,2-3,7-8H2,1H3/t12-,13+,14+ checkY
  • Key:MNJNPLVXBISNSX-WDNDVIMCSA-N checkY

参考资料

  1. ^ 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. 1987, 92 (4): 520–3. PMID 3114804. S2CID 25814825. doi:10.1007/bf00176488. 
  2. ^ Homesley HD, Hahne WF, McLees B, et al. 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. April 1993, 16 (2): 175–9. PMID 8452114. S2CID 11733418. doi:10.1097/00000421-199304000-00020. 
  3. ^ 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. Clin. Exp. Res. October 2000, 24 (10): 1500–4. PMID 11045857. doi:10.1111/j.1530-0277.2000.tb04567.x. 
  4. ^ 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. February 2002, 159 (4): 341–50. PMID 11823886. S2CID 21614467. doi:10.1007/s00213-001-0939-4. 
  5. ^ Kos T, Popik P, Pietraszek M, et al. Effect of 5-HT3 receptor antagonist MDL 72222 on behaviors induced by ketamine in rats and mice. Eur Neuropsychopharmacol. May 2006, 16 (4): 297–310. PMID 16288851. S2CID 43575963. doi:10.1016/j.euroneuro.2005.10.001. 
  6. ^ 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. January 2008, 62 (1): 8–13. PMID 17948891. S2CID 20699645. doi:10.1002/syn.20461.