Literature DB >> 1511846

Effects of LP-805, a novel vasorelaxant agent, a potassium channel opener, on rat thoracic aorta.

K Kishii1, T Morimoto, N Nakajima, K Yamazaki, M Tsujitani, I Takayanagi.   

Abstract

1. In rat thoracic aorta, LP-805 (0.1-10 microM) caused the marked reduction of NE-induced maximum response and relaxed the low K+ (less than 35.9 mM)-induced contraction, in a concentration-dependent manner, but failed to relax the high K+ (65.9 mM)-induced contraction. 2. Glibenclamide (0.3-1 microM) caused a parallel shift of concentration-response curve produced by LP-805 for 25.9 mM K(+)-induced contraction and prevented the LP-805-induced reduction in maximum response evoked by NE in a concentration-dependent manner. 3. Glibenclamide (10 microM) prevented the LP-805 (10 microM)-induced decrease in cytosolic Ca2+ levels which was increased by 1 microM NE or 25.9 mM K+. 4. LP-805 (10 microM) increased basal 86Rb efflux, which was completely inhibited by 10 microM glibenclamide. 5. The results suggest that LP-805 causes a vasorelaxation as a consequence of the decrease in cytosolic Ca2+ levels due to the increase in K+ efflux via opening ATP-dependent K+ channels.

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Year:  1992        PMID: 1511846     DOI: 10.1016/0306-3623(92)90094-z

Source DB:  PubMed          Journal:  Gen Pharmacol        ISSN: 0306-3623


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