Jacobs A, Keatinge W R
Br J Pharmacol. 1974 Jul;51(3):405-11. doi: 10.1111/j.1476-5381.1974.tb10676.x.
1 Procaine in concentrations up to 20 mM facilitated or induced electrical and mechanical activity in arterial smooth muscle, even with tetrodotoxin present.2 Procaine (up to 20 mM) caused relaxation when electrical activity was blocked by prior potassium depolarization.3 Procaine (1 mM) reduced mechanical responses to noradrenaline (1 muM) which were not accompanied by action potentials. It generally reduced mechanical responses to noradrenaline (1 mM) while increasing electrical activity induced by this.4 Lignocaine (1 mM) did not facilitate electrical activity significantly; it relaxed arteries in saline or potassium-rich solution and reduced mechanical responses to noradrenaline.5 High concentrations of procaine (at least 80 mM) or lignocaine (at least 20 mM) blocked electrical activity and caused contraction followed by relaxation and complete unresponsiveness.
即使存在河豚毒素,浓度高达20 mM的普鲁卡因也能促进或诱导动脉平滑肌的电活动和机械活动。
当预先的钾离子去极化阻断电活动时,普鲁卡因(高达20 mM)会引起舒张。
普鲁卡因(1 mM)降低了对去甲肾上腺素(1 μM)的机械反应,这种反应不伴有动作电位。它通常会降低对去甲肾上腺素(1 mM)的机械反应,同时增加由此诱导的电活动。
利多卡因(1 mM)不会显著促进电活动;它使生理盐水或富含钾溶液中的动脉舒张,并降低对去甲肾上腺素的机械反应。
高浓度的普鲁卡因(至少80 mM)或利多卡因(至少20 mM)会阻断电活动,并引起收缩,随后是舒张和完全无反应状态。