ACTIONS OF PAPAVERINE, ASPAMINOL AND BILE SALTS AND INTRACELLULAR CYCLIC AMP LEVEL

概要

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Antioxytocin activities of bile salts and their effects on phosphodiesterase (PDE) activities and the intracellular level of cyclic AMP in the rat uterus were investigated, and the mode of action of the bile salts was compared with that of papaverine or Aspaminol. The bile salts, chenodesoxycholate, desoxycholate, ursodesoxycholate and cholate significantly decreased PDE activities and a good relationship between the PDE activities and the antioxytocin activities of the bile salts was observed. Chenodesoxycholate and desoxycholate significantly increased the intracellular level of cyclic AMP in the rat uterus. The exogenously applied CaCl<SUB>2</SUB> potentiated the inhibitory responses of the rat uterus to papaverine, aminophylline responses of the rat uterus to papaverine, aminophylline and bile salts, while the inhibitory response to Aspaminol was greatly reduced by excess CaCl<SUB>2</SUB>. These results indicate that the antioxytocin action of the bile salts may be exerted through an increase in the intracellular level of cyclic AMP. Further, the results support the theory that there are two mechanisms for “papaverine-like” antipasmodics.
社団法人日本薬理学会の論文