Agmo A, Paredes R
Eur J Pharmacol. 1985 Jun 19;112(3):371-8. doi: 10.1016/0014-2999(85)90783-6.
The GABAA agonists 3-amino-1-propanesulfonic acid and THIP reduced sexual behaviour in male rats only at relatively high doses, whereas baclofen produced an almost complete inhibition at a low dose (2.5 mg/kg). The GABA transaminase inhibitor aminooxyacetic acid had no effects, while gamma-acetylenic GABA produced a slight inhibition of sexual behaviour. The GABAA antagonist bicuculline had no effect. When THIP was administered concurrently with bicuculline, the former drug was potentiated. Therefore it is concluded that the GABAA receptor is not responsible for the inhibitory actions of THIP, and since baclofen was the most potent drug with regard to effects on sexual behaviour, it is suggested that the GABAB rather than the GABAA receptor is involved in the control of that behaviour. The slight effects of the transaminase inhibitors and the lack of effect of bicuculline suggest that the GABAergic neurons participating in the control of sexual activity are not tonically active. Finally, data are presented showing that the effects of GABAergic drugs on sexual behaviour are probably independent from those on locomotor activity.
γ-氨基丁酸A型（GABAA）激动剂3-氨基-1-丙磺酸和4,5,6,7-四氢异噁唑[5,4-c]吡啶-3-醇仅在相对高剂量时才会降低雄性大鼠的性行为，而巴氯芬在低剂量（2.5毫克/千克）时就产生了几乎完全的抑制作用。γ-氨基丁酸转氨酶抑制剂氨氧乙酸没有效果，而γ-乙炔基氨基丁酸对性行为有轻微抑制作用。GABAA拮抗剂荷包牡丹碱没有作用。当4,5,6,7-四氢异噁唑[5,4-c]吡啶-3-醇与荷包牡丹碱同时给药时，前一种药物的作用增强。因此得出结论，GABAA受体与4,5,6,7-四氢异噁唑[5,4-c]吡啶-3-醇的抑制作用无关，并且由于就对性行为的影响而言巴氯芬是最有效的药物，所以表明参与该行为控制的是GABAB而非GABAA受体。转氨酶抑制剂的轻微作用和荷包牡丹碱的无作用表明参与性活动控制的γ-氨基丁酸能神经元不是持续性活跃的。最后，给出的数据表明γ-氨基丁酸能药物对性行为的影响可能独立于其对运动活动的影响。
