Calixto J B, Antônio A
Gen Pharmacol. 1986;17(2):203-9. doi: 10.1016/0306-3623(86)90140-0.
The contractile responses of the isolated dog uterus to acetylcholine (Ach), oxytocin (Ot), histamine (Hist) and barium chloride (Ba2+) were non-competitively blocked by compound D600. This compound was significantly more potent against Ba2+-induced contractions. Increasing the calcium (Ca2+) concentration from 0.2 to 2.5 mM reverted the inhibitory effects of D600 against Ach, Ot, Hist and 1 mM Ba2+. The blockade produced by D600 against 30 mM Ba2+ was not reversed by increasing the Ca2+ concentration. In high K+-depolarizing solution, D600 produced a parallel and concentration-dependent displacement to the right to the concentration-response curves of both Ca2+ and Ba2+. The Schild plot yielded similar pA2 values for D600 against Ca2+ and Ba2+.
化合物D600对离体犬子宫对乙酰胆碱(Ach)、催产素(Ot)、组胺(Hist)和氯化钡(Ba2+)的收缩反应具有非竞争性阻断作用。该化合物对Ba2+诱导的收缩作用明显更强。将钙(Ca2+)浓度从0.2 mM提高到2.5 mM可逆转D600对Ach、Ot、Hist和1 mM Ba2+的抑制作用。D600对30 mM Ba2+产生的阻断作用不会因增加Ca2+浓度而逆转。在高钾去极化溶液中,D600使Ca2+和Ba2+的浓度-反应曲线平行且浓度依赖性地向右位移。Schild图显示D600对Ca2+和Ba2+的pA2值相似。