A peripherally acting opioid receptor antagonist (IC50s = 1.15

Naldemedine – 500 µg

Brand:
Cayman
CAS:
916072-89-4
Storage:
-20
UN-No:
Non-Hazardous - /

Naldemedine is a peripherally acting opioid receptor antagonist (IC50s = 1.15, 1.11, and 1.5 nM for recombinant human μ-, δ-, and κ-opioid receptors, respectively).{48812,48813} It inhibits opioid-induced emesis and vomiting in ferrets and opioid-induced constipation in rats (ED50 = 0.03 mg/kg for both) without affecting the analgesic effect of morphine in the tail-flick test in rats.{48812} Naldemedine induces the opioid withdrawal symptoms of diarrhea and teeth chattering, but not jumping, in morphine-dependent rats when administered at doses of 1 and 3 mg/kg, respectively.{48813} Formulations containing naldemedine have been used in the treatment of opioid-induced constipation.  

 

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SKU: 29570 - 500 µg Category:

Description

A peripherally acting opioid receptor antagonist (IC50s = 1.15, 1.11, and 1.5 nM for recombinant human μ-, δ-, and κ-opioid receptors, respectively); inhibits opioid-induced emesis and vomiting in ferrets and opioid-induced constipation in rats (ED50 = 0.03 mg/kg for both); induces the opioid withdrawal symptoms of diarrhea and teeth chattering, but not jumping, in morphine-dependent rats at 1 and 3 mg/kg, respectively

Formal name: (5α)-17-(cyclopropylmethyl)-6,7-didehydro-4,5-epoxy-3,6,14-trihydroxy-N-[1-methyl-1-(3-phenyl-1,2,4-oxadiazol-5-yl)ethyl]-morphinan-7-carboxamide

Synonyms:  S-297995

Molecular weight: 570.6

CAS: 916072-89-4

Purity: ≥95%

Formulation: A solid

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