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哌唑嗪对可卡因和右旋苯丙胺行为效应的拮抗作用。

Antagonism of the behavioral effects of cocaine and d-amphetamine by prazosin.

作者信息

Tessel R E, Barrett J E

出版信息

Psychopharmacology (Berl). 1986;90(4):436-40. doi: 10.1007/BF00174057.

DOI:10.1007/BF00174057
PMID:3101098
Abstract

Key pecking by pigeons was maintained under a 30-response fixed-ratio schedule of food delivery; lever pressing by squirrel monkeys was maintained under a 3-min fixed-interval schedule of food delivery. Administered alone, d-amphetamine (0.1-3.0 mg/kg), cocaine (1.0-3.0 mg/kg) and bupropion (1.0-30 mg/kg) either did not affect or decreased fixed-ratio responding of pigeons, whereas d-amphetamine (0.056-0.3 mg/kg) either increased or decreased (0.56 mg/kg) responding of monkeys maintained under the fixed-interval schedule. Prazosin, a selective centrally-active alpha 1 antagonist, produced a dose-dependent reversal of the rate-decreasing effects of d-amphetamine and cocaine but not of bupropion on fixed-ratio responding in pigeons. Prazosin also reversed both the rate-increasing and rate-decreasing effects of d-amphetamine on fixed-interval responding of squirrel monkeys. In contrast, the non-selective alpha-antagonist phentolamine enhanced d-amphetamine-induced decreases in fixed-ratio responding. These findings suggest that the behavioral effects of d-amphetamine and cocaine are produced at least in part by activation of central alpha 1 receptors. Prazosin may be a useful tool for better understanding the mechanisms through which cocaine, amphetamine, and other abused stimulant drugs exert their potent behavioral effects.

摘要

鸽子的啄键行为通过每30次反应给予一次食物的固定比率程序来维持;松鼠猴的杠杆按压行为通过每3分钟给予一次食物的固定间隔程序来维持。单独给药时,右旋苯丙胺(0.1 - 3.0毫克/千克)、可卡因(1.0 - 3.0毫克/千克)和安非他酮(1.0 - 30毫克/千克)要么不影响鸽子的固定比率反应,要么使其降低,而右旋苯丙胺(0.056 - 0.3毫克/千克)对按固定间隔程序维持的猴子的反应则要么增强要么降低(0.56毫克/千克)。哌唑嗪是一种选择性中枢活性α1拮抗剂,它能剂量依赖性地逆转右旋苯丙胺和可卡因对鸽子固定比率反应的速率降低作用,但不能逆转安非他酮的这种作用。哌唑嗪还能逆转右旋苯丙胺对松鼠猴固定间隔反应的速率增强和速率降低作用。相比之下,非选择性α拮抗剂酚妥拉明增强了右旋苯丙胺引起的鸽子固定比率反应的降低。这些发现表明,右旋苯丙胺和可卡因的行为效应至少部分是由中枢α1受体的激活产生的。哌唑嗪可能是一个有用的工具,有助于更好地理解可卡因、苯丙胺和其他滥用的兴奋剂药物发挥其强大行为效应的机制。

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ANTAGONISM OF A BEHAVIORAL EFFECT OF D-AMPHETAMINE BY CHLORPROMAZINE IN THE PIGEON.氯丙嗪对鸽子中右旋苯丙胺行为效应的拮抗作用
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氯氮平和哌唑嗪可减缓大鼠中由d-苯丙胺诱导的专注刻板行为期间的头部运动节奏。
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Review of the pharmacology and clinical profile of bupropion, an antidepressant and tobacco use cessation agent.安非他酮(一种抗抑郁药及戒烟药)的药理学与临床概况综述。
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Involvement of noradrenergic system in a remarkably rapid tongue clonus produced by acute hypnotic doses of ethanol in Fischer F344 rats.去甲肾上腺素能系统参与急性催眠剂量乙醇在Fischer F344大鼠中产生的显著快速的舌阵挛。
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Neuropharmacology. 1984 Nov;23(11):1241-51. doi: 10.1016/0028-3908(84)90040-6.