C25H27D5N2O4
货号:ajcx24224
CAS:N/A
分子式:C25H27D5N2O4
分子量：429.6
溶解度:DMSO: soluble,Methanol: soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Alvimopan-d₅is intended for use as an internal standard for the quantification of alvimopan by GC- or LC-MS. Alvimopan is a μ-opioid receptor antagonist (K_i= 0.47 nM).¹It is selective over the κ- and δ-opioid receptors (K_is= 100 nM and 12 nM, respectively). Alvimopan inhibits μ-opioid receptor-mediated GTP binding to CHO cell membranes with an IC₅₀value of 1.7 nM. It inhibits morphine-induced slowing of colorectal transit in mice with an ED₅₀value of 0.41 mg/kg.²Alvimopan (0.3 and 1 mg/kg, p.o.) reduces inhibition of gastrointestinal (GI) transit induced by morphine, but not apraclonidine , in rats. Formulations containing alvimopan have been used in the treatment of opioid-induced bowel dysfunction.

1.Le Bourdonnec, B., Barker, W.M., Belanger, S., et al.Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as μ opioid receptor antagonists with improved opioid receptor selectivity profilesBioorg. Med. Chem. Lett.18(6)2006-2012(2008) 2.Greenwood-Van Meerveld, B., Gardner, C.J., Little, P.J., et al.Preclinical studies of opioids and opioid antagonists on gastrointestinal functionNeurogastroenterol. Motil.16(Suppl. 2)46-53(2004)