The pharmacology of 20681-S and 20682-S, 6-oxo-N-cyclopropylmethylmorphinans, as narcotic antagonist analgesics.
Arch Int Pharmacodyn Ther
; 241(1): 79-91, 1979 Sep.
Article
en En
| MEDLINE
| ID: mdl-43119
It has been demonstrated that L-3hydroxy-6-oxo-N-cyclopropylmethylmorphinan methansulfonate (20681-S) and L-3,14-dihydroxy-6-oxo-N-cyclopropylmethylmorphinan methansulfonate (20682-S), have antinociceptive and narcotic antagonistic properties. In the rodent antinociceptive test, the action of 20681-S was more potent and of longer duration than that of morphine and of cyclazocine after subcutaneous or oral administration. The antinociceptive effect of 20682-S ranked between that of morphine and that of pentazocine in the mouse acetic acid-writhing test. Both compounds possessed potent narcotic antagonistic activities, 20682-S being more active than naloxone and oxilorphan and 20681-S being equipotent with cyclazocine. The latent side effects (respiratory depression and fall in blood pressure) and the acute toxicity of 20681-S and 20682-S, were less than those of reference narcotic antagonists or of narcotic antagonist analgesics.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Analgésicos
/
Morfinanos
/
Antagonistas de Narcóticos
Límite:
Animals
Idioma:
En
Revista:
Arch Int Pharmacodyn Ther
Año:
1979
Tipo del documento:
Article
Pais de publicación:
Bélgica