N-CHLOROACETYL 5-METHOXYTRYPTAMINE (ISAMIDE) - SELECTIVE ANTAGONIST OF 5-HYDROXYTRYPTAMINE IN THE RAT UTERUS
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Date
1979
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Abstract
Isamide, the N-chloracetyl derivative of 5-methoxytryptamine, produced a dose-dependent competitive blockade of uterine contractions in vitro induced by 5-HT [hydroxytryptamine]. The pA2 value for the 5-HT-isamide interaction was 4.42. The blockade was short-lasting and reversible; after recovery, a dose-dependent increase in the uterine sensitivity to 5-HT was found. The blockade was selective to the 5-HT receptor. The simultaneous application of 5-HT plus isamide partially prevented the 5-HT-induced auto blockade phenomenon. In addition, isamide did not affect the contractile responses of the uterus to oxytocin or bradykinin or the contractile effects of the rat vas deferens to adrenaline.