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DAGO([D-丙氨酸2,N-甲基苯丙氨酸4,甘醇]脑啡肽)可特异性逆转阿扑吗啡诱导的小鼠竖毛和梳理行为增加。

DAGO ([D-Ala2,N-Me-Phe4,Gly-ol]enkephalin) specifically reverses apomorphine-induced increase in rearing and grooming behaviors in the mouse.

作者信息

Ukai M, Toyoshi T, Kameyama T

机构信息

Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Meijo University, Nagoya, Japan.

出版信息

Brain Res. 1991 Aug 23;557(1-2):77-82. doi: 10.1016/0006-8993(91)90118-f.

Abstract

The effects of intracerebroventricular injections (10 microliters) of the mu-selective opioid peptide DAGO on apomorphine (0.1, 0.56, 1.0 and/or 3.0 mg/kg)-induced motor activity were investigated in the mouse using multi-dimensional behavioral analyses. A lower dose (0.1 mg/kg) of apomorphine failed to significantly affect motor activity, whilst higher doses (0.56, 1.0 and 3.0 mg/kg) of the drug produced a marked increase in linear locomotion, circling, rearing and/or grooming behaviors. DAGO (0.003 and 0.01 micrograms) did not significantly affect different behaviors. DAGO (0.01 micrograms) antagonized the apomorphine (1.0 mg/kg)-induced increase in behaviors such as rearing and grooming. However, DAGO (0.003 or 0.01 micrograms) did not affect behaviors induced by a 3.0 mg/kg dose of apomorphine. Furthermore, the effects of DAG]O on apomorphine-induced behaviors were fully reversed by treatment with the mu-selective alkylating agent beta-FNA (beta-funaltrexamine) (5.0 micrograms). These results suggest that mu opioid receptors play a principal role in the apomorphine-induced increase in rearing and grooming behaviors.

摘要

采用多维度行为分析方法,研究了向小鼠脑室内注射(10微升)μ-选择性阿片肽DAGO对阿扑吗啡(0.1、0.56、1.0和/或3.0毫克/千克)诱导的运动活动的影响。较低剂量(0.1毫克/千克)的阿扑吗啡未能显著影响运动活动,而较高剂量(0.56、1.0和3.0毫克/千克)的该药物则使直线运动、转圈、直立和/或梳理行为显著增加。DAGO(0.003和0.01微克)对不同行为没有显著影响。DAGO(0.01微克)拮抗了阿扑吗啡(1.0毫克/千克)诱导的诸如直立和梳理等行为的增加。然而,DAGO(0.003或0.01微克)并不影响3.0毫克/千克剂量阿扑吗啡诱导的行为。此外,用μ-选择性烷基化剂β-FNA(β-氟纳曲酮)(5.0微克)处理可完全逆转DAGO对阿扑吗啡诱导行为的影响。这些结果表明,μ阿片受体在阿扑吗啡诱导的直立和梳理行为增加中起主要作用。

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