Receptor specificity of the 5HT2 receptor antagonist, LY53857
Receptor specificity of the 5HT2 receptor antagonist, LY53857
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5HT2 受体拮抗剂 LY53857 的受体特异性
DOI：
10.1002/ddr.430050404
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发表时间：
1985
影响因子：
3.8
通讯作者：
L. Wittenauer
中科院分区：
文献类型：
--
作者：
Marlene L. Cohen;W. Colbert;L. Wittenauer
LY53857 是一种有效的血管 5HT2 受体拮抗剂，缺乏显着的 α1 或多巴胺拮抗剂活性。本报告研究了 LY53857 与其他受体机制的相互作用。 LY53857在豚鼠气管、豚鼠心房、豚鼠回肠或大鼠输精管中没有表现出激动剂活性。此外，LY53857 不会拮抗豚鼠气管中的组胺 (H1) 或 β2 受体、豚鼠心房中的 β1 受体、豚鼠回肠中的毒蕈碱或血管紧张素 I 受体。然而，LY53857 确实阻断了 α2 受体 (−log KB = 6.51)，这是通过选择性 β2 激动剂 UK-14,304 对豚鼠回肠抽搐反应的抑制作用的拮抗作用来确定的。 LY53857 拮抗 β2 受体的浓度比阻断 5HT2 受体所需的浓度高约 6000 倍 (−log KB = 10.3)。综合起来，这些数据支持这样的论点：LY53857 是 5HT2 受体的高度选择性拮抗剂，并且 LY53857 是探测 5HT2 受体和血清素能机制的有用工具。
LY53857 is a potent antagonist at vascular 5HT2 receptors that lacks prominent α1 or dopamine antagonist activity. The present report investigates the interaction of LY53857 with other receptor mechanisms. LY53857 showed no agonist activity in the guinea pig trachea, guinea pig atria, guinea pig ileum, or rat vas deferens. Furthermore, LY53857 did not antagonize histamine (H1) or β2 receptors in the guinea pig trachea, β1 in the guinea pig atria, muscarinic, or angiotensin I receptors in the guinea pig ileum. However, LY53857 did block α2 receptors (−log KB = 6.51) as determined by antagonism of the inhibitory effects of the selective β2 agonist, UK‐14,304, on the twitch response in the guinea pig ileum. LY53857 antagonized β2 receptors at concentrations approximately 6000‐fold higher than necessary to block 5HT2 receptors (−log KB = 10.3). Taken in concert, these data support the contention that LY53857 is a highly selective antagonist of 5HT2 receptors, and that LY53857 is a useful tool with which to probe 5HT2 receptors and serotonergic mechanisms.