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(3H)二氢烯丙洛尔与成年大鼠心脏分离细胞的β肾上腺素能受体的结合

Binding of (3H)dihydroalprenolol to beta adrenoceptors of cells isolated from adult rat heart.

作者信息

Moustafa E, Giachetti A, Downey H F, Bashour F A

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1978 May;303(1):107-9. doi: 10.1007/BF00496192.

Abstract

Myocardial cells isolated from adult rat heart bind (3H)dihydroalprenolol. Sixty-one percent of this binding appeared to be at the beta adrenoceptors since it was inhibited by saturating quantities of the beta antagonist propranolol or by the beta agonist isoprenaline. The binding is stereoselective as the l-isomer of isoprenaline caused greater inhibition than the d-isomer. The binding of (3H)dihydroalprenolol to beta adrenoceptors was saturable; half maximum binding occurred at about 8 nM and full saturation at 30--40nM.

摘要

从成年大鼠心脏分离出的心肌细胞能结合(3H)二氢阿普洛尔。这种结合的61%似乎是在β肾上腺素受体上,因为它被饱和量的β拮抗剂普萘洛尔或β激动剂异丙肾上腺素所抑制。由于异丙肾上腺素的l-异构体比d-异构体引起的抑制作用更强,所以这种结合具有立体选择性。(3H)二氢阿普洛尔与β肾上腺素受体的结合是可饱和的;半数最大结合发生在约8 nM处,完全饱和发生在30 - 40 nM处。

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