腺苷的心血管作用在大鼠和豚鼠中有所不同，但腺苷受体并无差异。

Cardiovascular actions of adenosines, but not adenosine receptors, differ in rat and guinea pig.

作者信息

Ueeda M, Thompson R D, Padgett W L, Secunda S, Daly J W, Olsson R A

机构信息

Department of Internal Medicine, University of South Florida, Tampa 33612.

出版信息

Life Sci. 1991;49(18):1351-8. doi: 10.1016/0024-3205(91)90199-l.

DOI:10.1016/0024-3205(91)90199-l

PMID:1921650

Abstract

This study compared the structure-activity relationships of 16 analogues at the A1 and A2 adenosine receptors (A1AR, A2AR) of rat and guinea pig. Radioligand binding studies revealed no marked differences in the affinities of each analogue at the A1AR of brain cortex or the A2AR of brain striatum. Bioassay employing Langendorff heart preparations showed that the guinea pig is more sensitive than the rat to A1AR-mediated slowing of conduction through the atrioventricular node and, in some instances, to A2AR-mediated coronary vasodilation. That difference could reflect factors such as receptor density or efficacy of coupling to effector systems.

摘要

本研究比较了16种类似物在大鼠和豚鼠A1和A2腺苷受体（A1AR、A2AR）上的构效关系。放射性配体结合研究表明，每种类似物在大脑皮层A1AR或脑纹状体A2AR上的亲和力没有显著差异。使用Langendorff心脏标本进行的生物测定表明，豚鼠比大鼠对A1AR介导的房室结传导减慢更敏感，在某些情况下，对A2AR介导的冠状动脉血管舒张也更敏感。这种差异可能反映了诸如受体密度或与效应系统偶联的效能等因素。