Ferrari F, Baggio G, Mangiafico V
Pharmacol Res Commun. 1986 Dec;18(12):1159-68. doi: 10.1016/0031-6989(86)90031-7.
Imidazole (IMID), (9.37-75 mg/Kg) and yohimbine (YOH), (0.5-2.5 mg/Kg), strongly potentiated lisuride-induced mounting, scored as a percentage of animals affected and mean number of mounts per animal, while clonidine (150 micrograms/Kg) significantly antagonized the phenomenon. A high (2 mg/Kg) but not a low (50 micrograms/Kg) dose of B-HT 920 and DPI (100 and 500 micrograms/Kg) also inhibited lisuride-induce mounting. While, at present, IMID specific activity on monaminergic system is not yet conclusive, it is demonstrated that, at the doses used, YOH and clonidine are selective alpha 2 antagonist and agonist, respectively; B-HT 920 preferentially stimulates D2 receptors at 50 micrograms/Kg and alpha 2 receptors at 2 mg/Kg; finally DPI, proposed as DAI agonist, also activates alpha 2 receptors. Therefore, in view of the dose-related receptorial selectivity of action of the drugs tested, neurochemical mechanisms on specific receptors involved for modulation of this form of sexual behaviour are briefly discussed.
咪唑(IMID)(9.37 - 75毫克/千克)和育亨宾(YOH)(0.5 - 2.5毫克/千克)能强烈增强利苏瑞ide诱导的爬跨行为,以受影响动物的百分比和每只动物的平均爬跨次数来评分,而可乐定(150微克/千克)则能显著拮抗这一现象。高剂量(2毫克/千克)而非低剂量(50微克/千克)的B - HT 920以及DPI(100和500微克/千克)也能抑制利苏瑞ide诱导的爬跨行为。虽然目前IMID对单胺能系统的特异性活性尚无定论,但已证明,在所使用的剂量下,YOH和可乐定分别是选择性α2拮抗剂和激动剂;B - HT 920在50微克/千克时优先刺激D2受体,在2毫克/千克时刺激α2受体;最后,被认为是DAI激动剂的DPI也能激活α2受体。因此,鉴于所测试药物作用的剂量相关受体选择性,简要讨论了参与调节这种性行为形式的特定受体上的神经化学机制。