In-vivo studies with the opioid antagonist, 16-methylcyprenorphine.
The effect of the opioid antagonist, 16-methylcyprenorphine (RX8008M), on the antinociceptive action of the mu-selective agonist, morphine, and the kappa-selective agonist, U50488H, has been investigated in the mouse abdominal constriction test. RX8008M produced a dose-dependent antagonism of the antinociceptive effect of morphine, but did not antagonize the response to U50488H. RX8008M should prove a useful probe for the in-vivo characterization of the receptor selectivity of opioid drugs.
D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D000700:Analgesics; D000818:Animals; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009019:Morphinans / Q000494:pharmacology*; D009020:Morphine / Q000037:antagonists & inhibitors; D009119:Muscle Contraction / Q000187:drug effects; D009292:Narcotic Antagonists / Q000494:pharmacology*; D011759:Pyrrolidines / Q000037:antagonists & inhibitors
D000700:Analgesics; D009019:Morphinans; D009292:Narcotic Antagonists; D011759:Pyrrolidines; C051207:16-methylcyprenorphine; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D009020:Morphine