Danthuluri N R, Deth R C
Biochem Biophys Res Commun. 1984 Dec 28;125(3):1103-9. doi: 10.1016/0006-291x(84)91397-4.
The influence of the phorbol ester, 12-o-tetradecanoylphorbol-13 acetate (TPA) on the contractility of rat and rabbit aorta was assessed. At 10(-8) to 10(-5)M TPA produced a gradual contraction of rat aorta, while rabbit aorta gave only a small contraction at 10(-5)M. Contractions were irreversible and dependent on extracellular Ca2+. Associated with TPA-induced contraction, alpha-adrenergic receptor responses of the rat were inhibited in a noncompetitive manner, while rabbit responses were little affected. Since TPA activates phospholipid-dependent protein kinase C in a manner analogous to endogenous diacylglycerol, a critical role for the latter in alpha-adrenergic events is suggested.
评估了佛波酯12 - O - 十四烷酰佛波醇 - 13 - 乙酸酯（TPA）对大鼠和兔主动脉收缩性的影响。在10⁻⁸至10⁻⁵M浓度下，TPA使大鼠主动脉逐渐收缩，而兔主动脉仅在10⁻⁵M时产生轻微收缩。收缩是不可逆的，且依赖于细胞外钙离子。与TPA诱导的收缩相关，大鼠的α - 肾上腺素能受体反应以非竞争性方式受到抑制，而兔的反应受影响较小。由于TPA以类似于内源性二酰基甘油的方式激活磷脂依赖性蛋白激酶C，提示后者在α - 肾上腺素能事件中起关键作用。
