Melchiorre C, Gallucci P
Farmaco Sci. 1983 Dec;38(12):950-6.
beta-Haloalkylamines bind at two sites on the adrenergic alpha-receptor, one related to the noradrenaline-recognition site and the other possibly concerned with the calcium channel. In order to verify whether this might apply to other alpha-blockers the tetramine disulfide benextramine was selected owing to its unprecedented covalent selectivity towards the adrenergic alpha-receptor. The fast acting beta-haloalkylamine DMPEA and the "classical" calcium antagonist verapamil were used for protection experiments against benextramine blockade of rat vas deferens adrenergic alpha-receptor. It was demonstrated that two target thiols are probably involved in benextramine binding and one of them might possibly be located at the periphery of, or masked within, the calcium channel which may be connected physiologically to the adrenergic alpha-receptor. However, the hypothesis that the present results could indicate the selective interaction of benextramine with two different subtypes of the adrenergic alpha-receptor is also discussed.
β-卤代烷基胺与肾上腺素能α受体的两个位点结合，一个位点与去甲肾上腺素识别位点相关，另一个位点可能与钙通道有关。为了验证这是否适用于其他α阻滞剂，选择了四胺二硫化物苄非他明，因为它对肾上腺素能α受体具有前所未有的共价选择性。速效β-卤代烷基胺DMPEA和“经典”钙拮抗剂维拉帕米用于大鼠输精管肾上腺素能α受体苄非他明阻断的保护实验。结果表明，两个靶硫醇可能参与苄非他明的结合，其中一个可能位于钙通道的外周或被掩盖在钙通道内，钙通道可能在生理上与肾上腺素能α受体相连。然而，也讨论了目前的结果可能表明苄非他明与肾上腺素能α受体的两种不同亚型选择性相互作用的假说。
