Kimball F A, Lauderdale J W, Nelson N A, Jackson R W
Prostaglandins. 1976 Dec;12(6):985-95. doi: 10.1016/0090-6980(76)90132-5.
The relative binding affinities for both the prostaglandin (PG)E1 and PGF2alpha specific bovine luteal binding sites were determined for five PGE and fourteen PGF derivatives and analogs. Relative binding affinity was determined in vitro using membranes prepared from bovine corpora luteal (CL) obtained from the slaughterhouse. The parent structure of the analog was a dominant feature in determining the affinity for the respective PG binding site. Luteolysis was determined in cattle following intramuscular injection of various doses of prostaglandin once between days 6 and 14 after estrus and measuring CL regression by ovarian palpation per rectum, interval between injection and return to estrus and duration of the subsequent estrous cycle. A dose which was luteolytic was established for each of eight PGF-type compounds, and a dose which was not luteolytic was also established. There appeared to be limited association between the relative affinity for the PGF2alpha specific site in vitro and the estimated luteolytic dose range of these PGF analogs when tested in cattle. Differences in in vivo luteolytic potency for the compounds tested could not be explained by differences in binding affinity. Differences in metabolism and absorption may also be important in the determination of in vivo potency.
测定了5种前列腺素E（PGE）衍生物和14种前列腺素F（PGF）衍生物及类似物对前列腺素E1（PGE1）和前列腺素F2α（PGF2α）特异性牛黄体结合位点的相对结合亲和力。使用从屠宰场获取的牛黄体（CL）制备的膜在体外测定相对结合亲和力。类似物的母体结构是决定其对相应前列腺素结合位点亲和力的主要特征。在发情后第6至14天之间，对牛进行一次肌肉注射不同剂量的前列腺素，然后通过直肠触诊卵巢来测量黄体退化情况、注射至发情回归的间隔时间以及随后发情周期的持续时间，以此来测定黄体溶解情况。确定了8种PGF型化合物各自的溶黄体剂量，同时也确定了非溶黄体剂量。在体外对PGF2α特异性位点的相对亲和力与这些PGF类似物在牛体内测试时的估计溶黄体剂量范围之间似乎关联有限。所测试化合物在体内的溶黄体效力差异无法通过结合亲和力的差异来解释。代谢和吸收的差异在体内效力的测定中可能也很重要。
