Effects of ovariectomy and ovarian steroids on binding of 3H-mepyramine, an H1-histamine antagonist, in rat hypothalamus.

The effects of ovariectomy and ovarian steroids on 3H-mepyramine binding, a histamine antagonist considered as a suitable ligand for H1-histamine receptors, were studied. Saturation binding assays and Scatchard plot analyses were performed in membranes from hypothalamus of adult female rats. In the hypothalamus of ovariectomized (OVX) rats, a decrease of the Bmax and a lowering of Kd values as compared to diestrous rats, were found. Estradiol administration to OVX rats as a single SC injection (25 micrograms), or by means of SC Silastic capsules (500 micrograms/ml estradiol benzoate; 10 mm/100 g b.wt.), reversed the effects of OVX, increasing both Bmax and Kd. The addition of progesterone (25 mg) blunted the effects of estradiol (50 micrograms). The present results suggest that hypothalamic H1-histamine receptors may be modulated by the ovarian steroids and provide further evidence of a possible role of histamine in female gonadotropin regulation.