Gonzalez M I, Patmore L, Wilson C A
Department of Obstetrics & Gynaecology, St. George's Hospital Medical School, London, UK.
Eur J Pharmacol. 1996 Sep 19;312(1):1-6. doi: 10.1016/0014-2999(96)00445-1.
The role of alpha 2-adrenoceptors in mediating the noradrenergic control of female sexual behaviour was investigated employing a selective alpha 2-adrenoceptor antagonist, delequamine (RS15385). The drug was given in graded doses of 0.01-30 mg/kg p.o. to ovariectomised plus adrenalectomised rats primed with either 2 micrograms oestradiol benzoate which yielded mainly non-receptive animals or 5 micrograms oestradiol benzoate followed 48 h later by 0.5 mg progesterone, which stimulated a high level of receptivity. Doses between 0.1 and 30 mg/kg significantly increased lordotic activity (receptivity) with an ED50 of 0.32 mg/kg, but had no effect on ear-wiggling or hopping-and-darting (proceptivity). Delequamine had no inhibitory effect in animals displaying high levels of receptivity. Thus we have shown a selective alpha 2-adrenoceptor antagonist, given orally, can stimulate female receptivity in a dose-dependent manner. Bilateral administration into the ventromedial nucleus, but not medial preoptic area, of delequamine (10 micrograms/side/rat) stimulated receptivity and it is suggested that the alpha 2-adrenoceptor may exert its effect by enhancing endogenous noradrenaline release at its active sites.
采用选择性α2-肾上腺素能受体拮抗剂地来夸明(RS15385),研究了α2-肾上腺素能受体在介导去甲肾上腺素能对雌性性行为控制中的作用。将该药物以0.01 - 30 mg/kg的分级剂量口服给予卵巢切除加肾上腺切除的大鼠,这些大鼠分别用2μg苯甲酸雌二醇预处理(主要产生无接受性的动物)或5μg苯甲酸雌二醇预处理,48小时后再给予0.5mg孕酮(刺激高水平的接受性)。0.1至30mg/kg的剂量显著增加了脊柱前凸活动(接受性),ED50为0.32mg/kg,但对耳部摆动或跳跃- darting(求爱性)没有影响。地来夸明对表现出高水平接受性的动物没有抑制作用。因此,我们已经表明,口服给予的选择性α2-肾上腺素能受体拮抗剂可以以剂量依赖的方式刺激雌性接受性。将地来夸明(10μg/侧/大鼠)双侧注入腹内侧核而非内侧视前区可刺激接受性,提示α2-肾上腺素能受体可能通过增强其活性部位的内源性去甲肾上腺素释放来发挥作用。