新型胆囊收缩素拮抗剂L364,718可消除蛙皮素诱导的伤害感受，但增强吗啡诱导的镇痛作用。

The novel CCK antagonist L364,718 abolished caerulein- but potentiates morphine-induced antinociception.

作者信息

Rattray M, Jordan C C, De Belleroche J

机构信息

Department of Biochemistry, Charing Cross and Westminster Medical School, London, U.K.

出版信息

Eur J Pharmacol. 1988 Jul 26;152(1-2):163-6. doi: 10.1016/0014-2999(88)90849-7.

DOI:10.1016/0014-2999(88)90849-7

PMID:3208830

Abstract

The novel CCK antagonist L364,718 was tested on caerulein- and morphine-induced antinociception in rat using the paw pressure test. Caerulein-induced antinociception (ED50 = 30 micrograms/kg) was significantly inhibited by L354,718 (200 micrograms/kg i.p.) which on its own did not affect paw pressure threshold. In contrast, morphine-induced antinociception was significantly potentiated by L364,718. Since L364,718 is highly selective for 'peripheral' receptors which are found in tissue such as pancreas and gallbladder and a few discrete areas of brain, this receptor is likely to be implicated in the antinociceptive effect of caerulein.

摘要

新型缩胆囊素拮抗剂L364,718通过爪部压力试验在大鼠身上测试了其对蛙皮素和吗啡诱导的抗伤害感受作用。L354,718（腹腔注射200微克/千克）显著抑制了蛙皮素诱导的抗伤害感受作用（半数有效量=30微克/千克），而其本身并不影响爪部压力阈值。相比之下，L364,718显著增强了吗啡诱导的抗伤害感受作用。由于L364,718对存在于胰腺、胆囊等组织以及大脑一些离散区域中的“外周”受体具有高度选择性，该受体可能与蛙皮素的抗伤害感受作用有关。