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喹那洛烷(LY163502),一种D2多巴胺受体激动剂,通过中枢作用促进雄性恒河猴的阴茎勃起。

Quinelorane (LY163502), a D2 dopamine receptor agonist, acts centrally to facilitate penile erections of male rhesus monkeys.

作者信息

Pomerantz S M

机构信息

Department of Physiology, University of Pittsburgh School of Medicine, PA 15261.

出版信息

Pharmacol Biochem Behav. 1991 May;39(1):123-8. doi: 10.1016/0091-3057(91)90408-t.

Abstract

The present study examined the effects of a specific D2 dopamine receptor agonist, quinelorane (LY163502), on male sexual responding of rhesus monkeys. The effects of quinelorane were assessed by observing the behavioral responses of male rhesus monkeys to a sexually receptive female monkey that they could see, hear, and smell, but not physically contact. Quinelorane (IM) treatment produced dose-dependent effects on male sexual responding. Penile erections and masturbation were markedly facilitated following treatment with either 2.5 or 5 micrograms/kg quinelorane. Higher doses of quinelorane (10 and 25 micrograms/kg) generally did not further augment sexual responding, but rather resulted in a return in sexual responding to control vehicle levels. Quinelorane had a biphasic effect on yawning behavior of the monkeys with low doses (2.5 and 5 micrograms/kg) facilitating yawning and high doses (25 micrograms/kg) inhibiting yawning. Quinelorane in the dose-range (1-25 micrograms/kg) being evaluated did not reliably influence stereotypic behavior. In order to determine whether quinelorane acts centrally or peripherally to stimulate male sexual behavior, the ability of the peripherally active dopamine antagonist, domperidone, and the centrally active dopamine antagonist, haloperidol, to block the facilitation of sexual behavior produced by quinelorane treatment was examined. Administration of domperidone (50-200 micrograms/kg) failed to block quinelorane's effects on sexual behavior, whereas treatment with haloperidol (5-20 micrograms/kg) prevented quinelorane from stimulating male sexual responding. These experiments provide further evidence that dopaminergic mechanisms may play a role in the regulation of male sexual behavior of rhesus monkeys and, in particular, demonstrate the sexual stimulant properties of agents that provide central stimulation to D2 dopamine receptor sites.

摘要

本研究考察了一种特定的D2多巴胺受体激动剂喹那洛尔(LY163502)对恒河猴雄性性行为反应的影响。通过观察雄性恒河猴对一只它们能够看到、听到和闻到,但无法进行身体接触的处于性接受期的雌性猴子的行为反应,来评估喹那洛尔的作用效果。喹那洛尔(肌肉注射)治疗对雄性性行为反应产生剂量依赖性效应。用2.5或5微克/千克喹那洛尔治疗后,阴茎勃起和自慰明显增加。更高剂量的喹那洛尔(10和25微克/千克)通常不会进一步增强性行为反应,反而导致性行为反应恢复到对照载体水平。喹那洛尔对猴子的打哈欠行为有双相作用,低剂量(2.5和5微克/千克)促进打哈欠,高剂量(25微克/千克)抑制打哈欠。在所评估的剂量范围(1 - 25微克/千克)内,喹那洛尔对刻板行为没有可靠影响。为了确定喹那洛尔是通过中枢还是外周作用来刺激雄性性行为,研究了外周活性多巴胺拮抗剂多潘立酮和中枢活性多巴胺拮抗剂氟哌啶醇阻断喹那洛尔治疗所产生的性行为促进作用的能力。给予多潘立酮(50 - 200微克/千克)未能阻断喹那洛尔对性行为的影响,而用氟哌啶醇(5 - 20微克/千克)治疗可阻止喹那洛尔刺激雄性性行为反应。这些实验进一步证明多巴胺能机制可能在恒河猴雄性性行为的调节中起作用,特别是证明了对D2多巴胺受体位点提供中枢刺激的药物的性刺激特性。

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