某些阿朴菲类生物碱及其氧化、去氢衍生物对M-胆碱受体的作用

EFFECTS OF SOME APORPHINES AND THEIR OXIGENATED, DEHYDROGENATED DERIVATIVES ON M-CHOLINERGIC RECEPTORS

某些双苄基异喹啉及原小檗碱等异喹啉生物碱对M-胆碱受体有较高的亲和力,如粉防已碱Ki为7.3×10-8mol/L。阿朴菲类生物碱亦属异喹啉类生物碱。

The affinities of aporphine alkaloids to M-cholinergic receptors were increased in parellel with the elevation of their oxidation state. The rank order of their affinities is as follows. Oxoaporphines were the highest, dehydroaporphines were the second and the original form of aporphines were the least in radioreceptor binding experiment. For example, oxocrebamine and dicentrinc (oxigenated form) exhibited the highest affinity with Ki values of 1.5×10^(-7) mol/L.Dehydrocrebamine and dehydro dicentrine (dehydrogenated form) with moderate oxidation state were lower than oxoaporphines but higher than original form of aporphines. The Ki values of dehydrocrebamine and dehydrodicentrine were 8.1×10^(-7) and 7.9×10^(-7) mol/L.The affinities of four of aporphines fell into the range of μmol/L.