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(±)-CP-96,345,一种NK1受体拮抗剂,在哺乳动物坐骨神经制备中具有局部麻醉样作用。

(+/-)-CP-96,345, an NK1 receptor antagonist, has local anaesthetic-like effects in a mammalian sciatic nerve preparation.

作者信息

Karlsson U, Näsström J, Berge O G

出版信息

Regul Pept. 1994 Jun 16;52(1):39-46. doi: 10.1016/0167-0115(94)90019-1.

Abstract

The effect of the non-peptide NK1 receptor antagonist (+/-)-CP-96,345 was investigated on the compound action potential (cAP) recorded in the isolated guinea-pig nerve, and compared to the effects of the local anaesthetic lidocaine and the L-type Ca2+ channel antagonist diltiazem. (+/-)-CP-96,345, as well as lidocaine and diltiazem, produced a concentration dependent reduction of the cAP amplitude. All three drugs showed frequency dependent block. The block of the cAP by lidocaine was fully reversible at all concentrations tested, while the block by (+/-)-CP-96,345 and diltiazem were only partly reversible at higher concentrations. The present findings indicate that (+/-)-CP-96,345 exerts a local anaesthetic-like effect on nerve conduction.

摘要

研究了非肽类NK1受体拮抗剂(±)-CP-96,345对分离的豚鼠神经中记录的复合动作电位(cAP)的影响,并与局部麻醉药利多卡因和L型Ca2+通道拮抗剂地尔硫卓的作用进行了比较。(±)-CP-96,345以及利多卡因和地尔硫卓均使cAP幅度呈浓度依赖性降低。所有三种药物均表现出频率依赖性阻滞。在所有测试浓度下,利多卡因对cAP的阻滞均可完全逆转,而(±)-CP-96,345和地尔硫卓在较高浓度下的阻滞仅部分可逆。目前的研究结果表明,(±)-CP-96,345对神经传导具有类似局部麻醉药的作用。

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