Wilson M A, Dwyer K D, Roy E J
Neural and Behavioral Biology Program, University of Illinois, Champaign 61820.
Brain Res Bull. 1989 Feb;22(2):181-5. doi: 10.1016/0361-9230(89)90040-3.
Tricyclic antidepressants such as imipramine interact with a membrane binding site associated with the uptake of serotonin. Ovarian hormones estradiol and progesterone were found to affect the concentration and affinity of imipramine binding sites in the hypothalamus but not the cortex of female rats. In vivo and in vitro, estradiol increased the amount of imipramine binding at physiological concentrations; at high concentrations estradiol decreased imipramine binding. Ovariectomy (OVX) had no effect on imipramine binding, consonant with the biphasic dose-response relationship for estradiol. The effects of progesterone were dependent upon the concentration of estradiol. Effects of physiological concentrations of both estradiol and progesterone on imipramine binding in an isolated membrane preparation suggest that the hormones are affecting this aspect of serotonergic neuronal function by nongenomic mechanisms.
三环类抗抑郁药如丙咪嗪可与一个与血清素摄取相关的膜结合位点相互作用。研究发现，卵巢激素雌二醇和孕酮会影响雌性大鼠下丘脑而非皮质中丙咪嗪结合位点的浓度和亲和力。在体内和体外实验中，生理浓度的雌二醇会增加丙咪嗪的结合量；高浓度时，雌二醇会降低丙咪嗪的结合量。卵巢切除术（OVX）对丙咪嗪结合无影响，这与雌二醇的双相剂量反应关系一致。孕酮的作用取决于雌二醇的浓度。生理浓度的雌二醇和孕酮对分离膜制剂中丙咪嗪结合的影响表明，这些激素通过非基因组机制影响血清素能神经元功能的这一方面。
