THE NK2 RECEPTOR ANTAGONIST SR48968 INHIBITS THALAMIC RESPONSES EVOKED BY THERMAL BUT NOT MECHANICAL NOCICEPTION

被引:28
作者
SANTUCCI, V
GUEUDET, C
EMONDSALT, X
BRELIERE, JC
SOUBRIE, P
LEFUR, G
机构
[1] Sanofi Recherche
关键词
NK2 RECEPTOR ANTAGONISTS; THALAMIC EXTRACELLULAR RECORDING; THERMAL NOCICEPTION;
D O I
10.1016/0014-2999(93)90104-P
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:143 / 146
页数:4
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