Petkov V, Todorov S, Georgiev V, Petkova B, Donev N
Acta Physiol Pharmacol Bulg. 1979;5(4):3-12.
Glaucine and the newly-synthesized compounds possess some general properties conditioned by the common apomorphine structure - inhibition of the central nervous system, brief decrease in blood pressure and spasmolytic action. At the same time the changes in the structure of glaucine lead to quantitative or qualitative changes in some of its effects. Substitution of hydrogen in 3rd position with -CH2. NH-group reduces glaucine toxicity 3.5 times. Still greater decrease in the toxicity (7.5-10 times) is found in the case of N-oxidation or dehydrogenation of glaucine. The extension of the methyl group in 3rd position with a hydroxy group or with an amide residue of the benzoic acid, as well as the dehydrogenation and N-oxidation of glaucine, lead to intensification of the inhibitory action on the central nervous system. With the exception of 7-methyl dehydroglaucine which has antitussive action similar to glaucine, the other glaucine structural analogues do not possess this property. Both glaucine and its structural analogues exercise a bronchoconstrictor effect. 3-Aminomethyl derivatives preserve the spasmolytic activity of glaucine, and their several-fold lower toxicity makes them more promising spasmolytic agents than glaucine. Dehydrogenation and N-oxidation of glaucine reduce considerably its spasmolytic action.
青藤碱及其新合成的化合物具有一些由共同的阿朴吗啡结构所决定的一般性质——抑制中枢神经系统、血压短暂下降以及解痉作用。同时，青藤碱结构的改变会导致其某些效应发生量变或质变。在第3位用-CH₂.NH-基团取代氢原子可使青藤碱毒性降低3.5倍。在青藤碱进行N-氧化或脱氢的情况下，毒性降低得更多（7.5至10倍）。在第3位用羟基或苯甲酸的酰胺残基延长甲基，以及青藤碱的脱氢和N-氧化，会导致对中枢神经系统抑制作用的增强。除了具有与青藤碱类似镇咳作用的7-甲基脱氢青藤碱外，其他青藤碱结构类似物不具有此性质。青藤碱及其结构类似物均具有支气管收缩作用。3-氨基甲基衍生物保留了青藤碱的解痉活性，且其毒性低几倍，使其成为比青藤碱更有前景的解痉剂。青藤碱的脱氢和N-氧化会大大降低其解痉作用。
