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KMID : 0376419940180010009
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Chonbuk University Medical Journal
1994 Volume.18 No. 1 p.9 ~ p.18
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Effect of KT-362 on the Release of 3H-Norepinephrine from Isolated Rat Atria
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유상은
곽용근/은홍배/김용기/김기원/조규박
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Abstract
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KT-362 (5[3[-2-(3, H-dimethoxyphenyl)-ethyl] amino]-1-oxopropyl)-2, 3, 4, 5-tetrahydro-1, 5-benzothiazepine fumarate) is one of the potential drugs that can be used in some of cardiovascular diseases such as arrhythmias, hypertension or
myocardiac
infarction. Recently it has been reported that KT-362 has inhibitory actions on intracellular Ca2+ release, Na+ influx and Ca2+ influx. However, the action of this drug on sympathetic activity is still unclear. In this study, effect of KT-362 on
the
release of 3H-NE from isolated rat atria preloaded with 3H-NE and its mechanism of action were investigated.
1. KT-362 elicited a dose-related increase in the release of 3H-NE.
2. The 3H-NE-releasing effect of KT-362 was not affected by LiCl2, 2, 3-dinitrophenol or yohimbine, but was potentiated by cocaine.
3. KT-362 inhibited H-NE uptake and 45Ca2+ uptake in naive or KC1-stimulated preparations.
4. KT-362 decreased tyramine-induced 3H-NE release, while reserpine diminished 3H-NE releasing effect of KT-362.
The above results indicate that KT-362 has augmentory action on NE release as well as inhibitory actions on NE-uptake and Ca2+-uptake, and that NE-releasing effect of KT-362 is due to the direct action on the catecholamine store.
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KEYWORD
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