ROLE OF NK1 TACHYKININ RECEPTORS IN THERMONOCICEPTION - EFFECT OF (+/-)-CP 96,345, A NONPEPTIDE SUBSTANCE-P ANTAGONIST, ON THE HOT PLATE TEST IN MICE

被引：65

作者：

LECCI, A ^{[1
]}

GIULIANI, S ^{[1
]}

PATACCHINI, R ^{[1
]}

VITI, G ^{[1
]}

MAGGI, CA ^{[1
]}

机构：

[1] MENARINI PHARMACEUT,DEPT CHEM RES,I-50131 FLORENCE,ITALY

来源：

NEUROSCIENCE LETTERS | 1991年 / 129卷 / 02期

关键词：

CP 96,345; SUBSTANCE-P; BOMBESIN; SPINAL CORD; HOT PLATE; MOUSE;

D O I：

10.1016/0304-3940(91)90485-C

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

We have tested the ability of (+/-)-CP 96,345, a novel nonpeptide substance P (SP) antagonist, to block the aversive behaviour induced by intrathecal (i.t.) administration of SP and to induce thermal antinociception in mice. (+/-)-CP 96,345 administered i.t. or i.p. selectively blocked the effect of i.t. SP while leaving the response to i.t. bombesin unaffected. At the same dose proven effective against i.t. SP, (+/-)-CP 96,345 produced thermal analgesia in the hot plate test (52-degrees-C). Using isolated organs for bioassay evaluation of activity at tachykinin receptor, (+/-)-CP 96,345 was found to be a potent (pA2 8.11, c.l. 7.9-8.3) and competitive NK1 receptor antagonist while it was devoid of activity at NK2 or NK3 receptors. These findings provide clear indication for the participation of SP, via NK1 receptors, in thermal nociception.

引用

页码：299 / 302

页数：4

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