β-Funaltrexamine (hydrochloride)

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A µ- and κ1-opioid receptor antagonist (Kis = 0.3 and 0.2 nM, respectively); selective for µ- and κ1-opioid receptors over the δ-opioid receptor (Ki = 12.8 nM); reversibly inhibits electricity-induced twitches of isolated guinea pig ileal longitudinal muscle strips (IC50 = 48 nM), indicating opioid agonist activity; inhibits endomorphin 1-induced conditioned place preference in mice at 0.3 µg/animal, i.c.v.; prevents decreases in urine output induced by fentanyl, D-propoxyphene, buprenorphine, profadol, or bromadoline in water-loaded rats at 40 mg/kg; reduces hemokinin 1-induced increases in the latency to withdrawal in the tail-flick test in mice