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Phasic and Tonic Components in 5-HT2 Receptor-Mediated Rat Aorta Contraction: Participation of Ca++ Channels and Phospholipase C(1)

机译:5-HT2受体介导的大鼠主动脉收缩中的阶段性和强直性成分:Ca ++通道和磷脂酶C的参与(1)

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The mechanisms of 5-hydroxytryptamine (5-HT)-induced contraction of rat aorta were investigated in vitro. The 5-HT-induced contraction could be analyzed into two distinct components (phasic and tonic) by the use of appropriate inhibitors; nifedipine, an inhibitor of voltage-dependent Ca(++) channels, inhibited only the phasic component of 5-HT-induced contraction while totally blocking the KCl-induced contraction. 2-Nitro-4-carboxyphenyl-N,N-diphenylcarbamate, an inhibitor of phospholipase C, inhibited the tonic components of 5-HT-induced contraction as well as the 5-HT-induced stimulation of phosphoinositide hydrolysis in rat aorta. This component of contraction was mimicked by a protein kinase C activator 12-O-tetradecanolyphorbol-13-acetate. These results suggest that 5-HT2 receptors differentially regulate a voltage-dependent Ca(++) channel and phospholipase C activity; the voltage-dependent Ca(++) channel is involved in the phasic component of contraction whereas the phosphoinositide hydrolysis that results in the activation of protein kinase C and calcium mobilization by inositol triphosphate plays a physiologically important role in the tonic component of the aortic contraction.

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