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苄基异喹啉类化合物拮抗钙调素(CaM),对环核苷酸磷酸二酯酶(CaM-PDE)产生抑制作用。它们的拮抗能力与分子中非极性端的疏水性相关,增强疏水性能增强拮抗性;极性端为叔胺或季铵离子时,抗CaM性基本不变;在受试的化合物中,D_3的抗CaM活性最强,IC_(50)值为2.8μmol/L。
Benzylisoquinolines antagonize calmodulin (CaM) and inhibit the cyclic nucleotide phosphodiesterase (CaM-PDE). Their antagonistic ability is related to the hydrophobicity of the non-polar end of the molecule, which enhances the hydrophobicity and enhances the antagonism. When the polar end is the tertiary amine or the quaternary ammonium ion, the anti-CaM property is basically unchanged. In the tested compounds, The strongest anti-CaM activity, IC 50 value was 2.8μmol / L.