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标题：Effects of Nanomolar to Submillimolar Carteolol on Noradrenaline Release in the Absence and Presence of Uptake1 and Uptake2 Blockers in Guinea Pig Pulmonary Arteries
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作者：Naoko MATSUSHITA ; Misako KUWAHARA ; Yoshio GOSHIMA 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1992
卷号：15
期号：12
页码：687-692
DOI：10.1248/bpb1978.15.687
出版社：The Pharmaceutical Society of Japan
摘要：Effects of nanomolar to submillimolar carteolol, a non-selective β-antagonist, on the evoked release at 1 Hz and the spontaneous release in the absence and presence of uptake₁ and uptake₂ blockers were studied in pulmonary arteries, isolated from guinea pigs, and then preloaded with [³H] noradrenaline. dl-Carteolol at 10^-8, 10^-7 and 10^-6 M applied at the increasing concentrations inhibited the evoked [³H]-release in untreated arteries and in desipramine and corticosterone-treated arteries. The spontaneous [³H]-release slightly but significantly increased or tended to increase in untreated arteries. dl-Carteolol at 10^-5 and 10^-4 M clearly and concentration-dependently increased the spontaneous [³H]-release in untreated and cocaine-treated arteries. This increase was markedly inhibited by further pretreatment with normetanephrine. The evoked [³H]-release was not altered by dl-carteolol at 10^-5 M, but increased at 10^-4 M. This increase was not modified by cocaine and by cocaine and normetanephrine. d-Carteolol at 10^-5 and 10^-4 M produced effects similar to those of dl-carteolol. Nanomolar to micromolar dl-carteolol inhibits the evoked [³H]-release, which supports our previous conclusion that this inhibition is due to blockade of tonically functioning presynaptic β₂-adrenoceptors. Carteolol at the higher concentrations seems to become a substrate for an uptake₂ mechanism and to produce an unknown sympathomimetic activity in guinea pig pulmonary arteries.
关键词：guinea pig pulmonary artery