SR 57227A is a partial agonist/partial antagonist of 5-HT3 receptor and inhibits subsequent 5-HT- or SR 57227A-induced 5-HT3 receptor current.
SR 57227A is a partial agonist/partial antagonist of 5-HT3 receptor and inhibits subsequent 5-HT- or SR 57227A-induced 5-HT3 receptor current.
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SR 57227A 是 5-HT3 受体的部分激动剂/部分拮抗剂，并抑制随后的 5-HT 或 SR 57227A 诱导的 5-HT3 受体电流。
DOI：
10.1016/j.bbrc.2018.11.174
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发表时间：
2019
影响因子：
3.1
通讯作者：
Shimada S.
中科院分区：
文献类型：
--
作者：
Nakamura Y;Kondo M;Koyama Y;Shimada S.
血清素（5-羟色胺）3型（5-HT 3）受体是跨膜配体门控离子通道。尽管几种5-HT 3受体激动剂已被用作临床前工具，但SR 57227 A是最常用的5-HT 3受体激动剂，具有穿过血脑屏障的能力。然而，SR 57227 A的确切药理学特征仍不清楚。因此，我们检查了SR 57227 A在5-HT 3A和5-HT 3AB受体上的药理学特征。我们将人5-HT 3A互补RNA（cRNA）或人5-HT 3A和人5-HT 3AB cRNA的组合注射到非洲爪蟾（Xenopus laevisoocytes）细胞中，并在SR 57227 A存在下进行了5-HT 3A和5-HT 3AB受体电流的双电极电压钳记录。结果表明，SR 57227 A对5-HT 3受体具有部分激动/部分拮抗作用。有趣的是，SR 57227 A特异性降低5-HT或SR 57227 A诱导的后续电流幅度。基于其5-HT 3受体部分激动剂/部分拮抗剂的性质，我们预测SR 57227 A具有5-羟色胺稳定剂的功能。
The serotonin (5-hydroxytryptamine) type 3 (5-HT3) receptors are transmembrane ligand-gated ion channels. Although several 5-HT3receptor agonists have been used as preclinical tools, SR 57227A is the most commonly used 5-HT3receptor agonist with the ability to cross the blood brain barrier. However, the precise pharmacological profile of SR 57227A remains unclear. Therefore, we examined the pharmacological profile of SR 57227A at the 5-HT3A and 5-HT3AB receptors. We microinjectedXenopus laevisoocytes with human 5-HT3A complementary RNA (cRNA) or a combination of human 5-HT3A and human 5-HT3AB cRNA and performed two electrode voltage clamp recordings of 5-HT3A and 5-HT3AB receptor current in the presence of SR 57227A. Results showed that SR 57227A acts as partial agonist/partial antagonist at the 5-HT3receptor. Interestingly, SR 57227A specifically reduced subsequent current amplitudes induced by 5-HT or SR 57227A. Based on its 5-HT3receptor partial agonist/partial antagonist properties, we predict that SR 57227A functions as a serotonin stabilizer.