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Proc Soc Exp Biol Med ; 148(2): 443-8, 1975 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-1168347

RESUMEN

A rabbit liver enzyme system was used to produce the 6beta-OH reduced metabolites of naloxone and naltrexone. GC analysis indicated the presence of some 6alpha-OH metabolite in these samples. The narcotic antagonist activity of these 6beta-OH metabolite samples were compared to naloxone, naltrexone and standard 6alpha-OH naltrexone (EN-2260A) using the jumping response of morphine pellet implanted mice. For the naloxone series, the potencies were: Naloxone greater than EN 2265A greater than 6 beta-OH maloxone. For the naltrexone series: Naltrexone greater than EN 2260A greater than beta-OH naltrexone. The low potency of the reduced metabolites the rapid onset of action of the parent compounds militate against the formation of these metabolites contributing substantially to the overall narcotic antagonist action of the parent compounds.


Asunto(s)
Conducta Animal/efectos de los fármacos , Dependencia de Morfina/metabolismo , Actividad Motora/efectos de los fármacos , Naloxona/análogos & derivados , Naloxona/metabolismo , Antagonistas de Narcóticos/metabolismo , Animales , Cromatografía de Gases , Ciclopropanos/análogos & derivados , Ciclopropanos/farmacología , Relación Dosis-Respuesta a Droga , Humanos , Hígado/metabolismo , Espectroscopía de Resonancia Magnética , Masculino , Ratones , Naloxona/farmacología , Antagonistas de Narcóticos/farmacología
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