Formulation: A solid
Formal Name: 4-[[(5α,6β)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-yl]amino]-4-oxo-2-butenoic acid, methyl ester, monohydrochloride
Purity: ≥95%
Formula Markup: C25H30N2O6 • HCl
Formula Weight: 491
Shelf life (days): 1460
CAS Number: 72786-10-8
Notes: β-Funaltrexamine is an irreversible μ- and κ1-opioid receptor antagonist (Kis = 0.3 and 0.2 nM, respectively).{41323,69732} It is selective for μ- and κ1-opioid receptors over the δ-opioid receptor (Ki = 12.8 nM).{41323} β-Funaltrexamine also reversibly inhibits electricity-induced twitches of isolated guinea pig ileal longitudinal muscle strips (IC50 = 48 nM), indicating opioid agonist activity.{69732} In vivo, β-funaltrexamine (0.3 µg/animal, i.c.v.) inhibits conditioned place preference induced by the μ-opioid receptor agonist endomorphin 1 (Item No. 23280) in mice.{43256} It prevents decreases in urine output induced by the opioid agonists fentanyl, D-propoxyphene, buprenorphine, profadol, or bromadoline in water-loaded rats when administered at a dose of 40 mg/kg.{32325} β-Funaltrexamine also reduces hemokinin 1-induced increases in the latency to withdrawal in the tail-flick test in mice.{61982}
English
Deutsch
