Formulation: A solid
Formal Name: N-[2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-(phenyl-d5)propyl]-glycine
Purity: ≥99% deuterated forms (d1-d5)
Formula Markup: C25H27D5N2O4
Formula Weight: 429,6
Shelf life (days): 1460
Notes: Alvimopan-d5 is intended for use as an internal standard for the quantification of alvimopan (Item No. 23902) by GC- or LC-MS. Alvimopan is a μ-opioid receptor antagonist (Ki = 0.47 nM).{25494} It is selective over the κ- and δ-opioid receptors (Kis= 100 nM and 12 nM, respectively). Alvimopan inhibits μ-opioid receptor-mediated GTP binding to CHO cell membranes with an IC50 value of 1.7 nM. It inhibits morphine-induced slowing of colorectal transit in mice with an ED50 value of 0.41 mg/kg.{39510} Alvimopan (0.3 and 1 mg/kg, p.o.) reduces inhibition of gastrointestinal (GI) transit induced by morphine, but not apraclonidine (Item No. 23904), in rats. Formulations containing alvimopan have been used in the treatment of opioid-induced bowel dysfunction.
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