Smith E R, Stoker D, Kueny T, Davidson J M, Hoffman B B, Clark J T
Department of Molecular and Cellular Physiology, Stanford University School of Medicine, CA 94305, USA.
Pharmacol Biochem Behav. 1995 Jun-Jul;51(2-3):439-42. doi: 10.1016/0091-3057(95)00004-g.
We have previously reported that administration of racemic mixtures of propranolol was associated with a marked inhibition of mating behavior in male rats. To compare the effects of (+)-propranolol, (-)-propranolol, and (+/-)-propranolol in sexually experienced males, rats ejaculating in four or more mating tests were divided into three groups (N = 16 per group) such that no differences in parameters of copulatory behavior were evidence in preexperimental tests. No major effect of propranolol on parameters of behavior associated with initiation of sexual behavior was evident. In contrast, other measures of behavior were profoundly modified. The ejaculatory threshold, indicated by the number of intromissions preceding ejaculation, was increased after (+)- and (+/-)-propranolol, but not (-)-propranolol. The number of mounts without intromission preceding ejaculation was increased only after (+/-)-propranolol. A decrease in copulatory efficacy was evident after (-)- or (+/-)-propranolol, but not after (+)-propranolol. Increases in ejaculation latency, intercopulatory interval, and postejaculatory interval were observed after (-)- and (+/-)-propranolol, but not after (+)-propranolol. In summary, the present data indicate that the (-) isomer of propranolol is the active form necessary for the inhibitory effects of propranolol on male sexual function. We suggest that this inhibition is due to specific receptor-mediated mechanisms, involving beta-adrenoceptors and 5-HT1A receptor interactions.
我们之前报道过,给予普萘洛尔消旋混合物会显著抑制雄性大鼠的交配行为。为了比较(+)-普萘洛尔、(-)-普萘洛尔和(±)-普萘洛尔对有性经验雄性大鼠的影响,将在四次或更多次交配试验中射精的大鼠分为三组(每组N = 16),以使交配行为参数在实验前测试中无差异。普萘洛尔对与性行为启动相关的行为参数没有明显影响。相比之下,其他行为指标则有显著改变。射精阈值由射精前的插入次数表示,(+)-普萘洛尔和(±)-普萘洛尔给药后射精阈值升高,而(-)-普萘洛尔给药后则未升高。仅在给予(±)-普萘洛尔后,射精前无插入的爬跨次数增加。(-)-普萘洛尔或(±)-普萘洛尔给药后交配效率明显降低,而(+)-普萘洛尔给药后则未降低。(-)-普萘洛尔和(±)-普萘洛尔给药后射精潜伏期、交配间期和射精后间期均延长,而(+)-普萘洛尔给药后则未延长。总之,目前的数据表明,普萘洛尔的(-)异构体是普萘洛尔对雄性性功能产生抑制作用所必需的活性形式。我们认为这种抑制作用是由于特定的受体介导机制,涉及β-肾上腺素能受体和5-HT1A受体相互作用。