肾上腺素对豚鼠心房节前β-肾上腺素能受体的激活作用。
Adrenaline activation of prejunctional beta-adrenoceptors in guinea-pig atria.
作者信息
Majewski H, McCulloch M W, Rand M J, Story D F
出版信息
Br J Pharmacol. 1980;71(2):435-44. doi: 10.1111/j.1476-5381.1980.tb10956.x.
Abstract
- Adrenaline in a concentration of 1.0 microM depressed the stimulation-induced efflux of tritium from the guinea-pig atria incubated with [3H]-noradrenaline, whereas adrenaline in a concentration of 0.5 nM significantly enhanced the stimulation-induced efflux of tritium. This enhancement was blocked by metoprolol (0.1 microM) and thus appears to be mediated by beta-adrenoceptors. 2. In guinea-pig atria incubated with unlabelled adrenaline and then with [3H]-noradrenaline, both catecholamines were released by field stimulation. In such atria metoprolol, practolol, oxprenolol or propranolol decreased the stimulation-induced efflux of tritium. These effects did not occur if the atria were incubated with unlabelled noradrenaline and then with [3H]-noradrenaline, suggesting that neuronally released adrenaline activates prejunctional beta-adrenoceptors. 3. The effect of oxprenolol in decreasing the release of tritium from guinea-pig atria, incubated with unlabelled adrenaline and then with [3H]-noradrenaline was greater in the presence of phentolamine. This may reflect the alpha-adrenoceptor blocking activity of oxprenolol.
摘要
- 浓度为1.0微摩尔的肾上腺素抑制了用[3H]-去甲肾上腺素孵育的豚鼠心房中刺激诱导的氚流出，而浓度为0.5纳摩尔的肾上腺素显著增强了刺激诱导的氚流出。这种增强被美托洛尔（0.1微摩尔）阻断，因此似乎是由β-肾上腺素能受体介导的。2. 在先用未标记的肾上腺素孵育然后用[3H]-去甲肾上腺素孵育的豚鼠心房中，两种儿茶酚胺都通过场刺激释放。在这样的心房中，美托洛尔、普拉洛尔、氧烯洛尔或普萘洛尔减少了刺激诱导的氚流出。如果心房先用未标记的去甲肾上腺素孵育然后用[3H]-去甲肾上腺素孵育，则不会出现这些效应，这表明神经释放的肾上腺素激活了突触前β-肾上腺素能受体。3. 在存在酚妥拉明的情况下，氧烯洛尔减少先用未标记的肾上腺素孵育然后用[3H]-去甲肾上腺素孵育的豚鼠心房中氚释放的作用更大。这可能反映了氧烯洛尔的α-肾上腺素能受体阻断活性。
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Regulation of norepinephrine release from cardiac sympathetic fibers in the dog by presynaptic alpha- and beta-receptors.犬心脏交感神经纤维中去甲肾上腺素释放受突触前α和β受体的调节。
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