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软体动物主动脉球中的章鱼胺受体:氯氮平和杀虫脒的作用

Octopamine receptors in the molluscan aortic bulb: effects of clozapine and chlordimeform.

作者信息

Dougan D F, Wade D N

出版信息

Comp Biochem Physiol C Comp Pharmacol Toxicol. 1985;82(1):193-7. doi: 10.1016/0742-8413(85)90228-2.

Abstract

The presence of specific, stereo-selective octopamine receptors has been demonstrated in the non-spontaneously beating accessory ventricle (aortic bulb) of the clam Tapes watlingi. Analogues of octopamine with a single chloro group in either the para or meta positions of the benzene ring were 10 times less potent than octopamine in their agonist activity. In low concentrations (less than 200 microM), phentolamine, chlordimeform and clozapine were octopamine antagonists. In high concentrations (greater than 200 microM), clozapine, clonidine and chlordimeform induced changes in aortic tone similar to that produced by p-octopamine. This activity may result from the chloro-substituted phenamidine skeleton in both clozapine and chlordimeform.

摘要

已在菲律宾蛤仔非自发性搏动的副心室(主动脉球)中证实存在特异性、立体选择性的章鱼胺受体。在苯环的对位或间位带有单个氯基团的章鱼胺类似物,其激动剂活性比章鱼胺低10倍。在低浓度(小于200微摩尔)时,酚妥拉明、杀虫脒和氯氮平是章鱼胺拮抗剂。在高浓度(大于200微摩尔)时,氯氮平、可乐定和杀虫脒引起的主动脉张力变化类似于对章鱼胺所产生的变化。这种活性可能源于氯氮平和杀虫脒中氯取代的苯脒骨架。

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