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氯贝酸类似物的对映体对大鼠骨骼肌氯离子通道具有相反的作用。

Enantiomers of clofibric acid analogs have opposite actions on rat skeletal muscle chloride channels.

作者信息

Conte-Camerino D, Mambrini M, DeLuca A, Tricarico D, Bryant S H, Tortorella V, Bettoni G

机构信息

Medicinal Chemistry Department, Faculty of Pharmacy, University of Bari, Italy.

出版信息

Pflugers Arch. 1988 Nov;413(1):105-7. doi: 10.1007/BF00581238.

Abstract

The S-(-) isomers of a series of clofibric acid analogs produced only a block of chloride conductance of rat skeletal muscle fibers with increasing concentrations until block was nearly complete. The R-(+) isomers, on the other hand, at low concentrations increased chloride conductance by as much as 9% to 39% and at higher concentrations decreased chloride conductance, but never by more than 27% of the control value. The actions of the enantiomeric pairs to either produce or inhibit myotonic excitability paralleled their ability to block or increase chloride conductance, respectively.

摘要

一系列氯贝酸类似物的S-(-)异构体随着浓度增加仅对大鼠骨骼肌纤维的氯电导产生阻滞作用,直至阻滞几乎完全。另一方面,R-(+)异构体在低浓度时可使氯电导增加多达9%至39%,而在高浓度时则降低氯电导,但降低幅度从未超过对照值的27%。对映体对产生或抑制肌强直兴奋性的作用分别与其阻滞或增加氯电导的能力平行。

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