SCH 23390在血管平滑肌和大脑中的5-羟色胺受体拮抗剂特性。

5HT-receptor antagonist properties of SCH 23390 in vascular smooth muscle and brain.

作者信息

Hicks P E, Schoemaker H, Langer S Z

出版信息

Eur J Pharmacol. 1984 Oct 15;105(3-4):339-42. doi: 10.1016/0014-2999(84)90628-9.

Abstract

The dopamine D1-receptor antagonist SCH 23390 was a potent competitive antagonist of 5HT-induced vasoconstriction in the isolated perfused rat tail artery preparation (pA2 8.17) but a very weak antagonist of phenylephrine-induced responses (pA2 5.94). In rat brain cerebral cortex, SCH 23390 inhibited 5-HT2-sensitive [3H]spiperone binding with an IC50 of 112 nM. Binding of [3H]5HT to 5HT1 receptors in the cortex was inhibited by SCH 23390 with an IC50 of 2.49 microM. SCH 23390 has significant affinity for 5HT receptors in addition to the reported selective dopamine D1-receptor antagonist properties.

摘要

多巴胺D1受体拮抗剂SCH 23390在离体灌注大鼠尾动脉标本中是5-羟色胺（5HT）诱导的血管收缩的强效竞争性拮抗剂（pA2为8.17），但对去氧肾上腺素诱导的反应是非常弱的拮抗剂（pA2为5.94）。在大鼠脑皮质中，SCH 23390抑制5-HT2敏感的[3H]螺哌隆结合，IC50为112 nM。SCH 23390抑制皮质中[3H]5HT与5HT1受体的结合，IC50为2.49 microM。除了已报道的选择性多巴胺D1受体拮抗剂特性外，SCH 23390对5HT受体也有显著亲和力。