钙和Bay K 8644对雌激素在大鼠子宫中抑制作用的差异效应。

Differential effect of calcium and Bay K 8644 on the inhibitory action of estrogens in the rat uterus.

Fernandez A I, Martinez V, Cantabrana B, Hidalgo A

Departamento de Medicina, Facultad de Medicina, Universidad de Oviedo, Spain.

Gen Pharmacol. 1992 May;23(3):549-54. doi: 10.1016/0306-3623(92)90126-5.

Abstract

The effects of the estrogens estradiol (E2, 10(-7) to 3 x 10(-5) M) and diethylstilbestrol (DES, 10(-7) to 3 x 10(-6) M) on tonic contractions of the rat uterus induced by KCl and CaCl2 have been studied. 2. E2 and DES relaxed, in a dose-dependent way, the tonic contraction induced by KCl (60 mM) (IC50: 5.16 +/- 1.49 x 10(-6) and 4.51 +/- 0.03 x 10(-7) M); the tonic contraction induced by CaCl2 (3 mM) in the rat uterus incubated in depolarizing Krebs (127 mM of K+) have also been relaxed (IC50: 8.6 +/- 0.03 x 10(-7) and 2.56 +/- 0.07 x 10 M) by both drugs. 3. The CaCl2 (0.1 to 10 mM) counteracted the relaxing effect of E2 and DES, respectively, up to 28.13 +/- 10.2% and 34.71 +/- 11.5%, on KCl-induced contractions, and up to 126.36 +/- 19.35% and 95.8 +/- 16.3% on CaCl2-induced contractions. 4. Bay K 8644 (10(-10) to 10(-6) M) reversed the relaxing effect of E2 and DES, respectively, up to 42.49 +/- 2.28% and 43.31 +/- 3.59% on KCl-induced contractions, and up to 21.73 +/- 4.16% and 75.97 +/- 9.63% on CaCl2-induced contractions. 5. Propranolol (10(-6) M) did not modify the relaxing effect of E2 or DES on CaCl2-induced contractions.

摘要

研究了雌激素雌二醇（E2，10⁻⁷至3×10⁻⁵M）和己烯雌酚（DES，10⁻⁷至3×10⁻⁶M）对氯化钾和氯化钙诱导的大鼠子宫强直性收缩的影响。2. E2和DES以剂量依赖性方式松弛了由氯化钾（60 mM）诱导的强直性收缩（IC50：5.16±1.49×10⁻⁶和4.51±0.03×10⁻⁷M）；两种药物也松弛了在去极化的克雷布斯液（127 mM钾离子）中孵育的大鼠子宫由氯化钙（3 mM）诱导的强直性收缩（IC50：8.6±0.03×10⁻⁷和2.56±0.07×10 M）。3. 氯化钙（0.1至10 mM）分别抵消了E2和DES对氯化钾诱导收缩的松弛作用，最高可达28.13±10.2%和34.71±11.5%，对氯化钙诱导收缩的抵消作用最高可达126.36±19.35%和95.8±16.3%。4. 贝前列素K 8644（10⁻¹⁰至10⁻⁶M）分别逆转了E2和DES对氯化钾诱导收缩的松弛作用，最高可达42.49±2.28%和43.31±3.59%，对氯化钙诱导收缩的逆转作用最高可达21.73±4.16%和75.97±9.63%。5. 普萘洛尔（10⁻⁶M）未改变E2或DES对氯化钙诱导收缩的松弛作用。