佛波酯增强大鼠乳头肌中α1-肾上腺素能受体介导的正性肌力作用。
Phorbol ester potentiates alpha 1-adrenoceptor-mediated positive inotropic effect in rat papillary muscle.
作者信息
Otani H, Otani H, Das D K
机构信息
Department of Surgery, University of Connecticut School of Medicine, Farmington 06032.
出版信息
Jpn J Pharmacol. 1987 Nov;45(3):425-8. doi: 10.1254/jjp.45.425.
Tumor-promoting phorbol esters may alter alpha 1-adrenoceptor-mediated cardiac response by stimulating protein kinase C activity. We investigated the effect of phorbol-12,13-dibutyrate (PDBu) on the positive inotropic effect (PIE) in rat left ventricular papillary muscle. PDBu (1-100 nM) potentiated the phenylephrine (PE)-induced PIE in a dose- and time-dependent manner. The PIE induced by PE and PDBu was abolished by pretreatment with 3 x 10(-7) M prazosin. PDBu also enhanced PE-induced slow responses 2- to 3-fold. These results suggest that PDBu enhances alpha 1-adrenoceptor-mediated PIE by potentiating slow Ca2+ channels, presumably through the activation of protein kinase C.
促肿瘤佛波酯可能通过刺激蛋白激酶C活性来改变α1 - 肾上腺素能受体介导的心脏反应。我们研究了佛波醇 - 12,13 - 二丁酸酯（PDBu）对大鼠左心室乳头肌正性肌力作用（PIE）的影响。PDBu（1 - 100 nM）以剂量和时间依赖性方式增强去氧肾上腺素（PE）诱导的PIE。用3×10（-7）M哌唑嗪预处理可消除PE和PDBu诱导的PIE。PDBu还使PE诱导的慢反应增强2至3倍。这些结果表明，PDBu可能通过激活蛋白激酶C增强慢钙通道，从而增强α1 - 肾上腺素能受体介导的PIE。
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