Bade S C, Gardner R M
Biol Reprod. 1985 Jun;32(5):1031-7. doi: 10.1095/biolreprod32.5.1031.
Mepacrine is a potent inhibitor of uterine contractile responses in vitro. Pretreatment of isolated rat uterine horns with mepacrine (1.3 X 10(-4)M) for periods of time ranging from 15 s to 5 min prior to the addition of carbachol (1.0 X 10(-4)M) showed that mepacrine could significantly reduce carbachol-induced uterine contractile responses within 15 s of exposure. The maximal inhibitory effects of mepacrine on uterine contractile responses were observed within 2 min of mepacrine treatment. A dose-response study related to the effect of increasing concentrations of mepacrine (7.5 X 10(-6) to 1.3 X 10(-4)M) on carbachol-induced (1 X 10(-4)M) uterine contractions revealed that a dose of 3.1 X 10(-5)M mepacrine reduced the carbachol-induced contraction by 50%. A dose of 7.8 X 10(-5)M mepacrine produced the maximal inhibitory effect on the carbachol-induced uterine contractions. Two doses of mepacrine (3.1 X 10(-5) and 1.3 X 10(-4)M) significantly reduced maximal contractile responses and shifted contractile dose-response curves of carbachol, oxytocin, prostaglandin F2 alpha, and BaCl2 to the right. Based on the nonselective inhibition by mepacrine of contractile responses induced by different uterotonic agents, these results suggest that mepacrine cannot be used to characterize the role of phospholipase in regulating the actions of hormones in uterine tissue.
奎宁是体外子宫收缩反应的强效抑制剂。在加入卡巴胆碱（1.0×10⁻⁴M）之前，用奎宁（1.3×10⁻⁴M）对离体大鼠子宫角进行15秒至5分钟的预处理，结果表明，奎宁在暴露15秒内就能显著降低卡巴胆碱诱导的子宫收缩反应。奎宁处理2分钟内观察到其对子宫收缩反应的最大抑制作用。一项关于增加奎宁浓度（7.5×10⁻⁶至1.3×10⁻⁴M）对卡巴胆碱诱导（1×10⁻⁴M）子宫收缩影响的剂量反应研究表明，3.1×10⁻⁵M的奎宁剂量可使卡巴胆碱诱导的收缩降低50%。7.8×10⁻⁵M的奎宁剂量对卡巴胆碱诱导的子宫收缩产生最大抑制作用。两剂量的奎宁（3.1×10⁻⁵和1.3×10⁻⁴M）显著降低了最大收缩反应，并使卡巴胆碱、催产素、前列腺素F2α和氯化钡的收缩剂量反应曲线右移。基于奎宁对不同子宫收缩剂诱导的收缩反应的非选择性抑制作用，这些结果表明奎宁不能用于表征磷脂酶在调节子宫组织中激素作用方面的作用。
