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Life Sci ; 39(2): 127-33, 1986 Jul 14.
Artículo en Inglés | MEDLINE | ID: mdl-3014250

RESUMEN

The effects of the d- and l-isomers of pentazocine were compared to that of racemic pentazocine on contractions of the mouse isolated vas deferens. L-pentazocine inhibited electrically evoked contractions of the mouse vas deferens (MVD) in a dose-dependent manner (ID50 0.37 +/- 0.04 microM). In contrast, d-pentazocine augmented field stimulated contractions dose-dependently; per cent increases in contractions at 10 and 30 microM were 57.8 +/- 18.0 and 98.0 +/- 15.1%, respectively. Racemic pentazocine produced an intermediate effect between the two isomers. The effect of 1-pentazocine was antagonized by naloxone, whereas that of d-pentazocine was not. L-pentazocine did not effect the response of the MVD to exogenous norepinephrine at any concentration tested, while d-pentazocine depressed the response of the MVD to exogenous norepinephrine at one dose (0.3 microM). These findings demonstrate that d- and l-pentazocine produce opposite effects on the MVD. The effects of l-pentazocine are opioid mediated, while those of d-pentazocine are not. In the racemic mixture the opposing effects of the two isomers modulate each other, resulting in a diminished effect.


Asunto(s)
Pentazocina/farmacología , Receptores Opioides/efectos de los fármacos , Conducto Deferente/efectos de los fármacos , Animales , Estimulación Eléctrica , Masculino , Ratones , Contracción Muscular/efectos de los fármacos , Naloxona/farmacología , Norepinefrina/farmacología , Estereoisomerismo
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