A μ-opioid receptor antagonist (Ki = 0.47 nM); selective over κ- and δ-opioid receptors (Kis= 100 nM and 12 nM

Alvimopan – 5 mg

Brand:
Cayman
CAS:
156053-89-3
Storage:
-20
UN-No:
Non-Hazardous - /

Alvimopan is a peripherally acting μ-opioid receptor antagonist (Ki = 0.47 nM) that is selective over the κ- and δ-opioid receptors (Kis= 100 nM and 12 nM, respectively).{25494} In vitro, alvimopan inhibits μ-opioid receptor-mediated GTP binding to CHO cell membranes with an IC50 value of 1.7 nM. Alvimopan reduces morphine-induced inhibition of gastrointestinal (GI) transit in rats, guinea pigs, and mice more potently than methylnaltrexone (Item No. 24072) or naloxone (Item No. 15594).{39510} It inhibits morphine-induced slowing of colorectal transit in mice with an ED50 value of 0.41 mg/kg. Orally administered alvimopan (0.3 and 1 mg/kg, p.o.) reduces the inhibition of GI transit induced by morphine (Item No. ISO60147) but not by apraclonidine (Item No. 23904) in rats, suggesting that alvimopan does not act in the CNS. Formulations containing alvimopan have been used to treat opioid-induced bowel dysfunction.  

 

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Description

A μ-opioid receptor antagonist (Ki = 0.47 nM); selective over κ- and δ-opioid receptors (Kis= 100 nM and 12 nM, respectively); inhibits μ-opioid receptor mediated GTP binding to CHO cell membranes (IC50 = 1.7 nM); inhibits morphine-induced slowing of colorectal transit in mice (ED50 = 0.41 mg/kg, p.o.); antagonizes morphine-but not apraclonidine-induced inhibition of GI transit in rats (0.3 and 1 mg/kg, p.o.)

Formal name: N-[(2S)-2-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-1-oxo-3-phenylpropyl]-glycine

Synonyms:  ADL 8-2698|LY246736

Molecular weight: 424.5

CAS: 156053-89-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research

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