Opioid activity of lefetamine.
In mice lefetamine, at the dose of 50 mg/kg produces motor hyperactivity and at the dose of 60 mg/kg produces analgesia. Both effects are abolished by naloxone. Displacement studies by using [3H]-Naloxone (Nx), [3H]-D-Ala-Met-Enkephalinamide (DAMA) and [3H]-Ethylketocyclazocine (EKC) showed that lefetamine competes with all these opiates with an affinity 50 times lower than that of morphine. The displacing capacity of lefetamine is decreased in the presence of 50 mM Na+. It is concluded that lefetamine is an opioid agonist.
De Montis
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Devoto
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Bucarelli
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Tagliamonte
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D000779:Anesthetics, Local / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D003496:Cyclazocine / Q000031:analogs & derivatives / Q000494:pharmacology; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives / Q000378:metabolism; D016314:Ethylketocyclazocine; D007928:Lethal Dose 50; D008297:Male; D008691:Methadone / Q000494:pharmacology; D051379:Mice; D009020:Morphine / Q000494:pharmacology; D009270:Naloxone / Q000494:pharmacology; D010627:Phenethylamines / Q000378:metabolism / Q000494:pharmacology* / Q000633:toxicity; D051381:Rats; D011919:Rats, Inbred Strains; D011930:Reaction Time / Q000187:drug effects; D011957:Receptors, Opioid / Q000187:drug effects*
D000779:Anesthetics, Local; D010627:Phenethylamines; D011957:Receptors, Opioid; D009270:Naloxone; C011896:lephetamine; D004744:Enkephalin, Methionine; D016314:Ethylketocyclazocine; C022118:enkephalinamide-Met, Ala(2)-; D009020:Morphine; D003496:Cyclazocine; D008691:Methadone