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激动剂和拮抗剂与β-肾上腺素能受体的体外相互作用。

In vitro interactions of agonists and antagonists with beta-adrenergic receptors.

作者信息

Abramson S N, Molinoff P B

出版信息

Biochem Pharmacol. 1984 Mar 15;33(6):869-75. doi: 10.1016/0006-2952(84)90440-4.

Abstract

Neurotransmitters and hormones mediate their effects through interaction with specific receptors. A complete understanding of the effects of these chemical signals requires detailed knowledge, at the molecular level, of agonist/receptor interactions. It is likely that agonists and antagonists interact with the same site on a receptor. Agonists, however, are by definition different from antagonists in that agonists are responsible for transducing information across the cell membrane, ultimately resulting in a biological response, while antagonists appear to act through passive occupancy of receptors. Implicit in this concept is the idea that these fundamental differences between agonists and antagonists arise from the sequelae induced by agonist-specific interactions with receptors.

摘要

神经递质和激素通过与特定受体相互作用来介导其效应。要全面理解这些化学信号的作用,需要在分子水平上详细了解激动剂/受体相互作用。激动剂和拮抗剂可能与受体上的同一部位相互作用。然而,根据定义,激动剂与拮抗剂不同,因为激动剂负责跨细胞膜传递信息,最终导致生物学反应,而拮抗剂似乎是通过被动占据受体起作用。这一概念中隐含的观点是,激动剂和拮抗剂之间的这些根本差异源于激动剂与受体特异性相互作用所引发的后续效应。

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