Inagaki M, Hidaka H
Pharmacology. 1984;29(2):75-84. doi: 10.1159/000137995.
The ability of several calmodulin (CaM) antagonists, such as N-(6-aminohexyl)-5-chloro-1-naphthalene sulfonamide (W-7) and trifluoperazine, to displace [3H]-W-7 from CaM correlated with the inhibition of Ca2+-CaM-dependent phosphodiesterase (PDE) by these agents. These antagonists also suppressed the increase in fluorescence of n-phenyl-1-naphthylamine (NPN) by complex formation with CaM in the presence of Ca2+. However, the ability of some CaM antagonists, such as prenylamine and butaclamol, to displace [3H]-W-7 from CaM did not correlate with the inhibition of Ca2+-PDE. These antagonists enhanced the increase in fluorescence of NPN by complex formation with CaM in the presence of Ca2+. In a study employing 1H-nuclear magnetic resonance, the spectrum changes of the aromatic region of CaM induced by prenylamine were significantly more marked than the changes induced by W-7. These findings suggest two types of CaM antagonists. The compounds in each of the groups appear to have common molecular structures.
几种钙调蛋白（CaM）拮抗剂，如N-（6-氨基己基）-5-氯-1-萘磺酰胺（W-7）和三氟拉嗪，从CaM上置换[3H]-W-7的能力与这些药物对Ca2+-CaM依赖性磷酸二酯酶（PDE）的抑制作用相关。在Ca2+存在的情况下，这些拮抗剂还通过与CaM形成复合物抑制了N-苯基-1-萘胺（NPN）荧光的增加。然而，一些CaM拮抗剂，如普尼拉明和布他拉莫，从CaM上置换[3H]-W-7的能力与对Ca2+-PDE的抑制作用并不相关。在Ca2+存在的情况下，这些拮抗剂通过与CaM形成复合物增强了NPN荧光的增加。在一项使用1H-核磁共振的研究中，普尼拉明诱导的CaM芳香区光谱变化比W-7诱导的变化明显更显著。这些发现提示了两类CaM拮抗剂。每组中的化合物似乎具有共同的分子结构。
