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progesterone formed 8S and 5S binding complex, and the 3H-progesterone-8S binding was effectively inhibited by norethindrone or ethynodiol diacetate, resulting in the relative increases of 3H-progesterone-5S binding and free progesterone. The effect of steroids on progesterone-8S binding was studied by a double reciprocal plot which showed that the following steroids were competitive inhibitors for progesterone8S binding, and the order of the affinity for progesterone receptor was norethindrone (Ki= 2.3X 109 M) > 5a-dihydronorethindrone (Ki=6.0X10-9 M) > norethindrone acetate (Ki=8.8 X 10-9M) > lynestrenol (Ki=9.7X 109M) > 17a-ethyny1-4-estren-3g, 1713-diol (Ki=5.4X 10-8M) > ethynodiol diacetate (Ki=1.3X 10-7M), when taken from Ki. Ki (inhibitor constant) was calculated by the following equation: Ki=iKd/(Kp-Kd), where Kd is the dissociation constant, i is the concentration of an inhibitor and Kp is the pretending dissociation constant in the presence of an inhibitor. These results suggest that the 3-ketone and 1713-hydroxyl groups, and the plane of ring A/B of norethindrone are important to bind with progesterone receptor.

The interaction of progestogens of the estrane series with progesterone receptor in rabbit uterine cytosol