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Effects of iptakalim on intracellular calcium concentrations, PKA and PKC activities in rat tail artery smooth muscle cells / 药学学报
Acta Pharmaceutica Sinica ; (12): 954-957, 2005.
Artículo en Chino | WPRIM | ID: wpr-253533
ABSTRACT
<p><b>AIM</b>To investigate the effects of iptakalim, a new structural potassium channel opener (KCO), on intracellular calcium concentration ([Ca2+]i), protein kinase C (PKC), and cAMP-dependent kinase (PKA) activities in rat tail artery smooth muscle cells (RTA-SMC), and to analyze mechanisms involved in iptakalim reversing hypertensive vascular remodeling.</p><p><b>METHODS</b>RTA-SMC was cultured and passages 3-4 were used for experiment. [Ca2+] i was measured by laser scanning confocal microscope after loaded with fluorescent indicator fluo-3-acetoxymethylester, and activities of PKA and PKC were detected by commercial assay kits (the nonradioactive PepTag system) following instructions.</p><p><b>RESULTS</b>Compared with baseline, [Ca2+] i reduced significantly after iptakalim- or pinacidil-treatment at concentrations of 0.1, 1 and 10 micromol x L(-1), while diazoxide caused significant decrease at concentration of 1 and 10 micromol x L(-1). After preincubation with 1 micromol x L(-1) glibenclamide, [Ca2+] i was not significantly changed when iptakalim, pinacidil or diazoxide were added at concentration of 0.1 and 1 micromol x L(-1). Activities of PKA and PKC increased significantly by 1 micromol x L(-1) iptakalim- or pinacidil-treatment, while 1 micromol x L(-1) diazoxide induced significant change in activity of PKC but not in that of PKA.</p><p><b>CONCLUSION</b>The characteristics of iptakalim on [Ca2+] i, PKA and PKC are more or less similar to those of pinacidil. Iptakalim decreased [Ca2+] i while increased PKA and PKC activities of RTA-SMCs, which may contribute to its ability to reverse antihypertensive vascular remodeling.</p>
Asunto(s)
Texto completo: Disponible Índice: WPRIM (Pacífico Occidental) Asunto principal: Farmacología / Propilaminas / Cola (estructura animal) / Proteína Quinasa C / Células Cultivadas / Calcio / Ratas Sprague-Dawley / Proteínas Quinasas Dependientes de AMP Cíclico / Pinacidilo / Biología Celular Límite: Animales Idioma: Chino Revista: Acta Pharmaceutica Sinica Año: 2005 Tipo del documento: Artículo

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Texto completo: Disponible Índice: WPRIM (Pacífico Occidental) Asunto principal: Farmacología / Propilaminas / Cola (estructura animal) / Proteína Quinasa C / Células Cultivadas / Calcio / Ratas Sprague-Dawley / Proteínas Quinasas Dependientes de AMP Cíclico / Pinacidilo / Biología Celular Límite: Animales Idioma: Chino Revista: Acta Pharmaceutica Sinica Año: 2005 Tipo del documento: Artículo