Potency of L-364,718 as an antagonist of the behavioral effects of peripherally administered cholecystokinin.
Potency of L-364,718 as an antagonist of the behavioral effects of peripherally administered cholecystokinin.
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L-364,718 作为外周给药缩胆囊素行为效应拮抗剂的效力。
DOI：
10.1016/0024-3205(88)90678-9
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发表时间：
1988
期刊：
影响因子：
6.1
通讯作者：
J. Crawley
中科院分区：
文献类型：
--
作者：
S. Khosla;J. Crawley
发现一种新的外周胆囊收缩素受体拮抗剂L-364，718可阻断腹腔注射八肽硫酸胆囊收缩素引起的摄食量减少和探索活动减少。L-364，718在10 μg/kg - 10 mg/kg i. p.剂量下显著逆转胆囊收缩素诱导的摄食减少。L-364，718在500 ng/kg - 10 mg/kg i. p.剂量下显著逆转胆囊收缩素诱导的探索活动减少。718在腹膜内给药后即刻至90分钟。L-364，718在100 ng/kg-10 mg/kg i. p.剂量范围内单独给药时，对摄食量或探索活动无显著影响。作为外周给药胆囊收缩素行为效应的拮抗剂，该化合物的效力似乎至少比丙谷胺或苯并曲普强100倍。
A new antagonist of the peripheral cholecystokinin receptor, L-364,718, was found to block the reductions in food intake and exploratory activity induced by intraperitoneal administration of cholecystokinin octapeptide sulfate. L-364,718 significantly reversed the cholecystokinin-induced reduction in feeding at doses of 10 μg/kg - 10 mg/kg i.p. L-364,718 significantly reversed the cholecystokinin-induced reduction in exploratory activity at doses of 500 ng/kg - 10 mg/kg i.p. The time course of antagonist activity of L-364,718 was immediate to 90 minutes after intraperitoneal administration. L-364,718 had no significant effect on food intake or exploratory activity when administered alone, over the dose range of 100 ng/kg-10 mg/kg i.p. This compound appears to be at least one hundred times more potent than proglumide or benzotript as an antagonist of the behavioral effects of peripherally administered cholecystokinin.