Progestin Receptors in the Anterior Pituitary and Hypothalamus of Male Rats

In: International Journal of Andrology · 1978 · vol. 1(s2a) , pp. 175–183 · doi:10.1111/j.1365-2605.1978.tb00016.x · W2075645469
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Abstract

Properties of progestin receptors in the pituitary and hypothalamic cytosol fraction of male rats were studied using the highly potent progestin ( 3 H) R 5020 (17,20‐dimethyl‐19‐nor‐pregna‐4,9‐diene‐3,20‐dione). As shown by sucrose gradient analysis, specific binding of ( 3 H) R 5020 is associated with components migrating at 7 S and 4 S. The isoelectric point of the binding components were 5.8. The binding of ( 3 H) R 5020 is highly specific since it is easily displaced by unlabelled R 5020 and progesterone. The affinity of unlabelled testosterone, 17β‐estradiol and cyproterone acetate was much lower, whereas unlabelled cortisol had no affinity for the progestin receptor. The dissociation constant of pituitary R 5020 binding is approximately 1 times 10 ‐9 M. Pretreatment of the animals with 17β‐estradiol‐valerate greatly increased the progestin receptor levels in the tissues.

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