INTERACTION OF THE ANTIHYPERTENSIVE DRUG FELODIPINE WITH CALMODULIN
INTERACTION OF THE ANTIHYPERTENSIVE DRUG FELODIPINE WITH CALMODULIN
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DOI：
10.1038/292777a0
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发表时间：
1981-01-01
期刊：
影响因子：
64.8
通讯作者：
THULIN, E
中科院分区：
文献类型：
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作者：
BOSTROM, SL;LJUNG, B;THULIN, E
尽管它们的化学结构有显著的差异，但一组不同的药理药物被认为是专门阻止钙离子通过钙通道1内流，从而调节负性变力心脏作用和血管扩张。对心肌的电生理研究表明，慢内向钙电流被阻断，但这些药物在血管平滑肌中的细胞机制很大程度上是未知的。非洛地平[[4-(2，3-dichlorophenyl)-1，4-dihydropyridine-2，6-dimethyl 3，5-二羧酸-3-乙酯和5-甲酯]是一种新型的抗高血压药物，似乎能在活体内特异地扩张毛细血管前阻力血管。它是硝苯地平1和SKF 242602的结构类似物，这两种药物都被归类为钙拮抗剂，这意味着它们的血管和心肌作用是由于阻断钙内流所致。然而，这里报道的发现更多地指向非洛地平和钙结合蛋白(如钙调素)之间的相互作用。
Despite the marked differences in their chemical structure, members of a heterogeneous group of pharmacological agents are thought specifically to block Ca2+influx through calcium channels1and thus mediate negative inotropic cardiac effects and vasodilatation. Electrophysiological studies of the myocardium have shown that the slow inward Ca2+current is blocked1, but the cellular mechanism of these agents in vascular smooth muscle is largely unknown. Felodipine [4-(2,3-dichlorophenyl)-1,4-dihydropyridine-2,6-dimethyl 3,5-dicarboxylic 3-ethylester and 5-methylester)] is a new antihypertensive agent which seems specifically to dilate precapillary resistance vesselsin vivo.It is a structural analogue of nifedipine1and SKF 242602, both of which have been classified as ‘calcium antagonists’, implying that their vascular as well as myocardial actions are due to a blockade of Ca2+influx. However, the findings reported here point rather to an interaction between felodipine and calcium-binding proteins such as calmodulin.