盐酸苯乙哌啶和dl-15甲基PGF2α甲酯对大鼠卵巢黄体细胞的影响

盐酸苯乙哌啶(R1132)10μg/ml或dl-15甲基PGF_2α甲酯(PG05)5或10μg/ml在体外能明显抑制黄体细胞对hCG的反应性,使孕酮分泌下降。假孕大鼠po R1132 10 mg/kg或Sc PG 05 5.1 mg/kg不影响卵巢孕酮分泌,合并给药后却能使其降低。R1132无抗孕酮作用。卵巢分泌孕酮减少可能是抗早孕的主要原因.假孕大鼠po R1132 50 mg/kg或sc PG050.5 mg/kg可抑制卵巢腺苷环化酶的活性.该酶可能是R1132或PG05在大鼠抗早孕作用的重要靶酶。

EFFECTS OF DIPHENOXYLATE HYDROCHLORIDE AND dl-15 METHYL PROSTAGLANDIN F2a METHYL ESTER ON RAT LUTEAL CELLS

Diphenoxylate hydrochloride (R1132) at concentrations of 10 and 20 micrograms/ml or dl-15 methyl-PGF2 alpha methyl ester (PG05) at levels of 5 and 10 micrograms/ml was shown to have no effect on progesterone secretion by luteal cells in vitro in the absence of hCG. A marked increase in progesterone level was elicited by hCG as high as 3-8 fold the original value. The steroidogenic response of luteal cells to hCG was inhibited by R1132 and PG05. R1132 at a daily dose of 10 mg/kg or PG05 at a daily dose of 0.1 mg/kg for 5 days showed no obvious effect on ovary progesterone secretion in pseudopregnant rat. However, treatment with R1132 10 mg/kg plus PG05 0.1 mg/kg resulted in a decrease in the progesterone production of ovary in vitro. R1132 and PG05 at doses of 50 mg/kg and 0.5 mg/kg, respectively, exhibited an inhibitory effect on the adenylate cyclase activity.