Gupta C, Osterman J, Miljković M, Bardin C W
Steroids. 1977 May;29(5):669-77. doi: 10.1016/0039-128x(77)90018-6.
[3H]6alpha-methylprogesterone (6MP) was synthesized by selective catalytic tritiation of the delta1-olefinic bond of 6alpha-methylpregna-1,4-diene-3,20-dione. The metabolic clearance rate of 6MP (MCR6MP) was determined in 6 women by the single injection technique. The plasma MCR6MP was 4047 +/- 298 L/day (59 +/- 15 L/day/kg) which was higher than the MCR of progesterone and medroxyprogesterone acetate (6alpha-methyl-17alpha-hydroxy-pregna-4-ene-3,20-dione acetate). The high clearance was not due to binding or metabolism of 6MP by red cells. Although 6MP was bound to CBG with a lower affinity than progesterone, this could not entirely explain the high MCR6MP. When considered with the reports of progesterone and medroxyprogesterone acetate clearance, the present studies suggest that the 6alpha-substitution of progesterone leads to an increased rate of steroid metabolism in women.
通过对6α-甲基孕甾-1,4-二烯-3,20-二酮的δ1-烯键进行选择性催化氚化反应合成了[3H]6α-甲基孕酮（6MP）。采用单次注射技术测定了6名女性体内6MP的代谢清除率（MCR6MP）。血浆MCR6MP为4047±298升/天（59±15升/天/千克），高于孕酮和醋酸甲羟孕酮（6α-甲基-17α-羟基-孕甾-4-烯-3,20-二酮醋酸酯）的MCR。高清除率并非由于红细胞对6MP的结合或代谢所致。尽管6MP与皮质类固醇结合球蛋白（CBG）的结合亲和力低于孕酮，但这并不能完全解释高MCR6MP。结合孕酮和醋酸甲羟孕酮清除率的报告来看，目前的研究表明，孕酮的6α-取代导致女性体内类固醇代谢速率增加。
