Evaluation of the bronchodilator properties of Ro 31-6930, a novel potassium channel opener, in the guinea-pig
作者： P.M. Paciorek , I.S. Cowlrick , R.S. Perkins , J.C. Taylor , G.F. Wilkinson
DOI: 10.1111/J.1476-5381.1990.TB15797.X
关键词: Internal medicine 、 Potassium channel opener 、 Cromakalim 、 Bronchodilator 、 Endocrinology 、 Bronchodilator Agents 、 Salbutamol 、 Theophylline 、 Medicine 、 Leukotriene D4 、 Bronchoconstriction
摘要: 1. Ro 31-6930 (0.001-0.3 microM), cromakalim (0.03-3.0 salbutamol microM) and theophylline (0.3-100 evoked dose-related reductions in guinea-pig spontaneous tracheal tone with IC50 values of 0.044, 0.20, 0.021 21.0 microM respectively. All four agents also relaxed supported by betahistine, carbachol, 5-hydroxytryptamine (5-HT), leukotriene D4 (LTD4), U46619 prostaglandin D2 (PGD2). The order potency relaxants was always greater than theophylline. 2. 5-HT- histamine-induced bronchoconstriction pithed vagotomised guinea-pigs. dose producing 50% inhibition a 5-HT 11.6 micrograms kg-1 the histamine 4.4 kg-1. Salbutamol approximately 4-5 times more potent whilst 10 less as bronchodilator. Theophylline markedly any other agents. 3. 31-6930, cromakalim, each protected conscious guinea-pigs from respiratory distress. were effective at oral doses 1.0 3.0 mg 10.0 showed activity only 300 p.o. 4. is novel potassium channel opener which relaxant smooth muscle vitro bronchodilator vivo.
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