Chen D L, Chan W Y, Manning M
Department of Pharmacology, Cornell University Medical College, New York, NY 10021.
J Reprod Fertil. 1994 Nov;102(2):337-43. doi: 10.1530/jrf.0.1020337.
This paper describes further pharmacological characterization of the decidual prostaglandin-releasing oxytocin receptors and the myometrial uterotonic oxytocin receptors in the uterus of the pregnant rat. The effects of oxytocin, arginine-vasopressin and their related agonists and antagonists on the release of PGF2 alpha were studied in vitro on isolated uteri from rats on day 19-20 of pregnancy that had been incubated in Krebs buffer, pH 7.4, at 37 degrees C. The concentration of PGF2 alpha in the media was measured using specific radioimmunoassays. It was found that the decidual and myometrial oxytocin receptors exhibit different ligand specificities. Of the agonists tested, oxytocin and arginine-vasopressin stimulated PGF2 alpha release in a dose-dependent manner. Arginine-vasopressin has only 3% of the uterotonic potency of oxytocin, but was found to have 16% of its PGF2 alpha-releasing activity. [4-Threonine, 7-glycine]oxytocin, a highly potent and selective uterotonic oxytocin analogue, had no detectable prostaglandin-releasing activity at a dosage 30 times higher than oxytocin. However, 1-deamino-[8-D-arginine]vasopressin, a highly potent and selective antidiuretic arginine-vasopressin analogue, which has only 10% of the uterotonic activity of arginine-vasopressin, was as potent as arginine-vasopressin in prostaglandin-releasing activity.(ABSTRACT TRUNCATED AT 250 WORDS)
本文描述了妊娠大鼠子宫中蜕膜前列腺素释放型催产素受体和子宫肌层宫缩素催产素受体的进一步药理学特征。在体外，对妊娠第19 - 20天的大鼠离体子宫进行研究，这些子宫在pH 7.4的Krebs缓冲液中于37℃孵育，研究催产素、精氨酸加压素及其相关激动剂和拮抗剂对PGF2α释放的影响。使用特异性放射免疫分析法测量培养基中PGF2α的浓度。发现蜕膜和子宫肌层的催产素受体表现出不同的配体特异性。在所测试的激动剂中，催产素和精氨酸加压素以剂量依赖性方式刺激PGF2α释放。精氨酸加压素的宫缩效力仅为催产素的3%，但其PGF2α释放活性为催产素的16%。[4 - 苏氨酸，7 - 甘氨酸]催产素是一种高效且选择性的宫缩催产素类似物，在剂量比催产素高30倍时未检测到前列腺素释放活性。然而，1 - 脱氨基 - [8 - D - 精氨酸]加压素是一种高效且选择性的抗利尿精氨酸加压素类似物，其宫缩活性仅为精氨酸加压素的10%，但在前列腺素释放活性方面与精氨酸加压素一样有效。（摘要截短至250字）
