Alvimopan

Alvimopan is a µ-opioid receptor antagonist (Ki = 0.47 nM). It is selective over the kappa- and delta-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. Alvimopan (0.3 and 1 mg/kg, p.o.) reduces inhibition of gastrointestinal (GI) transit induced by morphine, but not apraclonidine (Cay-23904), in rats. Formulations containing alvimopan have been used in the treatment of opioid-induced bowel dysfunction.Formal Name: N-[(2S)-2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]-glycine. CAS Number: 156053-89-3. Synonyms: ADL 8-2698, LY246736. Molecular Formula: C25H32N2O4. Formula Weight: 424.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. SMILES: OC1=CC=CC([C@]2(C)CCN(C[C@@H](C(NCC(O)=O)=O)CC3=CC=CC=C3)C[C@@H]2C)=C1. InChi Code: InChI=1S/C25H32N2O4/c1-18-16-27(12-11-25(18,2)21-9-6-10-22(28)14-21)17-20(24(31)26-15-23(29)30)13-19-7-4-3-5-8-19/h3-10,14,18,20,28H,11-13,15-17H2,1-2H3,(H,26,31)(H,29,30)/t18-,20-,25+/m0/s1. InChi Key: UPNUIXSCZBYVBB-JVFUWBCBSA-N.