Alpha 2-adrenoceptor antagonists and male sexual behavior: I. Mating behavior

Three alpha 2-adrenoceptor antagonists yohimbine, idazoxan, and imiloxan were compared by examining the effects of a single injection on male rat copulatory behavior. Dose ranges were: yohimbine: 0.25-8.0 mg/kg; idazoxan: 0.25-8.0 mg/kg; imiloxan: 12.5-50.0 mg/kg. Yohimbine and idazoxan administration produced significant increases in the number of animals copulating to ejaculation and all three drugs increased the rate of copulation as evidenced by reductions in ejaculation latency and intercopulatory interval. Only yohimbine significantly reduced mount latency and postejaculatory interval, but yohimbine and imiloxan significantly reduced intromission latency and idazoxan showed a similar trend. The highest yohimbine dose suppressed sexual activity. A time-course experiment with yohimbine (2.0 mg/kg) and idazoxan (4.0 mg/kg) showed stimulation at 75 min and a trend at 5. To further explore the arousal-stimulating capacity of the two more effective drugs, a mounting test with genital anesthetization was used. Yohimbine but not idazoxan showed marked increases in mounting at 1.0-4.0 mg/kg. Both drugs had a suppressive effect at the highest doses. These data support the involvement of alpha 2-adrenoceptors in the regulation of male sexual behavior, specifically by facilitating sexual arousal, with no effects on ejaculatory threshold, as measured by intromission frequency. Yohimbine is the most globally effective agent and it is likely that factors other than yohimbine's alpha 2-antagonism may play a role in its unique, consistent and broad behavioral effects.