钙通道阻滞剂和沙丁胺醇对离体母马子宫的作用——与钙激动剂Bay K 8644的相互作用

Effect of calcium-channel blockers and salbutamol on the isolated mare uterus--interaction with the calcium agonist Bay K 8644.

作者信息

Coruzzi G, Poli E, Bertaccini G

机构信息

Institute of Pharmacology, Faculty of Veterinary, University of Parma, Italy.

出版信息

J Vet Pharmacol Ther. 1989 Dec;12(4):404-10. doi: 10.1111/j.1365-2885.1989.tb00691.x.

DOI:10.1111/j.1365-2885.1989.tb00691.x

PMID:2482371

Abstract

The effects of nifedipine, verapamil and diltiazem were investigated in the isolated mare uterus in comparison with salbutamol. All the calcium-channel blockers and salbutamol inhibited the spontaneous, KC1- and electrically induced contractions; nifedipine and salbutamol were the most potent compounds. The calcium agonist Bay K 8644 (10(-8)-10(-6) mol/l) competitively antagonized the inhibitory effect of nifedipine (pA2 value = 8.54 +/- 0.06), whereas it was only slightly or totally ineffective against verapamil, diltiazem and salbutamol. These results indicate that calcium-channel blockers are potent inhibitors of mare uterine motility in vitro and emphasize the importance of Ca2+-related mechanisms in the control of uterine smooth-muscle contractility. Moreover, the validity of Bay K 8644 as a tool to distinguish classes of calcium-channel antagonists is confirmed.

摘要

将硝苯地平、维拉帕米和地尔硫䓬与沙丁胺醇相比，研究了它们对离体母马子宫的作用。所有钙通道阻滞剂和沙丁胺醇均抑制自发性、氯化钾诱导和电诱导的收缩；硝苯地平和沙丁胺醇是最有效的化合物。钙激动剂Bay K 8644（10⁻⁸ - 10⁻⁶ mol/L）竞争性拮抗硝苯地平的抑制作用（pA₂值 = 8.54 ± 0.06），而对维拉帕米、地尔硫䓬和沙丁胺醇仅略有作用或完全无效。这些结果表明，钙通道阻滞剂是体外母马子宫运动的有效抑制剂，并强调了Ca²⁺相关机制在控制子宫平滑肌收缩性中的重要性。此外，证实了Bay K 8644作为区分钙通道拮抗剂类别的工具的有效性。