5 beta-Methyl-14 beta-(p-nitrocinnamoylamino)-7,8-dihydromorphinone: a long-lasting mu-opioid receptor antagonist devoid of agonist properties.
5 beta-Methyl-14 beta-(p-nitrocinnamoylamino)-7,8-dihydromorphinone (MET-CAMO) suppressed morphine-induced antinociception but had no effect on antinociception mediated by delta- or kappa-opioid receptors after a single i.c.v. 1-nmol injection from 8 to 72 h before testing. MET-CAMO had no agonist effects in the mouse tail-flick assay in doses up to 100 nmol. MET-CAMO is the first N-methylated morphine derivative which shows such long-lasting mu-selective opioid receptor antagonism with no agonistic properties.
Jiang
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Department of Pharmacology, University of Rochester, School of Medicine and Dentistry, NY 14642.
Sebastian
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A
Archer
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Bidlack
J M
JM
D000700:Analgesics / Q000494:pharmacology; D000818:Animals; D004091:Hydromorphone / Q000031:analogs & derivatives* / Q000494:pharmacology; D007276:Injections, Intraventricular; D051379:Mice; D009020:Morphine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D010147:Pain Measurement / Q000187:drug effects; D011930:Reaction Time / Q000187:drug effects; D017450:Receptors, Opioid, mu / Q000037:antagonists & inhibitors* / Q000187:drug effects
D000700:Analgesics; D017450:Receptors, Opioid, mu; C079551:5-methyl-14-(4-nitrocinnamoylamino)-7,8-dihydromorphinone; D009020:Morphine; D004091:Hydromorphone