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NK2受体拮抗剂SR48968可抑制热刺激而非机械性伤害性刺激诱发的丘脑反应。

The NK2 receptor antagonist SR48968 inhibits thalamic responses evoked by thermal but not mechanical nociception.

作者信息

Santucci V, Gueudet C, Edmonds-Alt X, Brelière J C, Soubrié P, Le Fur G

机构信息

Sanofi Recherche, Montpellier, France.

出版信息

Eur J Pharmacol. 1993 Jun 11;237(1):143-6. doi: 10.1016/0014-2999(93)90104-p.

Abstract

Extracellular recordings were made in the thalamic posterior nuclear group of anesthetized rats to study the effects of SR48968, a non-peptide NK2 receptor antagonist, on the responses evoked by thermal or mechanical nociceptive cutaneous stimulation. SR48968 (0.125-0.5 mg/kg, i.v. route) inhibited the responses to thermal stimulation while being ineffective on mechanically evoked responses in doses up to 2 mg/kg i.v. This effect was stereoselective since SR48965, the (R) enantiomer of SR48968 with a 2000-fold lower affinity for NK2 receptors, did not modify thermally evoked responses at a dose of 1 mg/kg i.v. These results support the notion that NK2 receptors are involved in thermal nociception.

摘要

在麻醉大鼠的丘脑后核群进行细胞外记录,以研究非肽类NK2受体拮抗剂SR48968对热或机械性伤害性皮肤刺激所诱发反应的影响。SR48968(0.125 - 0.5毫克/千克,静脉注射途径)抑制对热刺激的反应,而在静脉注射剂量高达2毫克/千克时对机械诱发反应无效。这种效应具有立体选择性,因为SR48968的(R)对映体SR48965对NK2受体的亲和力低2000倍,在静脉注射剂量为1毫克/千克时不改变热诱发反应。这些结果支持NK2受体参与热痛觉感受的观点。

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