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选择性阿片受体拮抗剂对布托啡诺诱导摄食的影响。

The effect of selective opioid antagonists on butorphanol-induced feeding.

作者信息

Levine A S, Grace M, Portoghese P S, Billington C J

机构信息

Research and Medicine Service, Veterans Administration Medical Center, Minneapolis, MN 55417.

出版信息

Brain Res. 1994 Feb 21;637(1-2):242-8. doi: 10.1016/0006-8993(94)91239-4.

Abstract

Butorphanol tartrate (BT) potently stimulates food intake in satiated rats. The opioid receptor profile of BT is complex and is dependent upon the assay and animal species studied. In the present study we utilized three selective opioid antagonists; namely beta-funaltrexamine (beta-FNA), naltrindole (NTI) and norbinaltorphimine (nor-BNI), to probe the opioid receptor profile of BT as an orexigenic agent. Intracerebroventricular administration of nor-BNI (kappa) antagonized the feeding effects of BT (8 mg/kg, s.c.) at doses of 1, 10 and 100 nmol at the 1-2 h time point and decreased feeding at all time points for the 10 nmol dose. After 1 h, the 100 nmol dose of nor-BNI decreased BT-induced feeding by about 72%. In contrast, intraventricular injection of only the highest dose of the selective mu opioid antagonist, beta-FNA (50 nmol), decreased BT-induced feeding. Intraventricular administration of the delta opioid agonist, NTI, failed to alter BT-induced feeding at doses as high as 50 nmol. These data suggest that BT is dependent upon the kappa and perhaps the mu opioid receptors to increase food intake in satiated rats.

摘要

酒石酸布托啡诺(BT)能有效刺激饱足大鼠的食物摄入量。BT的阿片受体谱较为复杂,且取决于所研究的实验方法和动物种类。在本研究中,我们使用了三种选择性阿片拮抗剂,即β-氟纳曲酮(β-FNA)、纳曲吲哚(NTI)和去甲丁丙诺啡(nor-BNI),来探究BT作为一种促食欲剂的阿片受体谱。脑室内注射nor-BNI(κ)在1至2小时时间点,剂量为1、10和100 nmol时,拮抗了BT(8 mg/kg,皮下注射)的进食作用,且10 nmol剂量在所有时间点均减少了进食。1小时后,100 nmol剂量的nor-BNI使BT诱导的进食减少了约72%。相比之下,仅脑室内注射最高剂量的选择性μ阿片拮抗剂β-FNA(50 nmol)可减少BT诱导的进食。脑室内注射δ阿片激动剂NTI,高达50 nmol的剂量未能改变BT诱导的进食。这些数据表明,BT在饱足大鼠中增加食物摄入量依赖于κ阿片受体,可能还依赖于μ阿片受体。

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