首页> 美国卫生研究院文献>British Journal of Pharmacology and Chemotherapy >Activation of prejunctional beta-adrenoceptors in rat atria by adrenaline applied exogenously or released as a co-transmitter.
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Activation of prejunctional beta-adrenoceptors in rat atria by adrenaline applied exogenously or released as a co-transmitter.

机译:肾上腺素对大鼠心房中结前β-肾上腺素受体的激活可以通过外源性肾上腺素应用或作为共递质释放。

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摘要

1 Adrenaline (10 nM) significantly enhanced the stimulation-induced efflux of radioactivity from rat atria previously incubated with [3H]-noradrenaline ([3H]-NA). This effect was abolished by metoprolol (.01 muM). 2 Adrenaline in a higher concentration (1 muM) and NA (1 muM) significantly reduced the stimulation-induced efflux of radioactivity. However, in the presence of phenoxybenzamine (10 muM), adrenaline (1 muM) enhanced the efflux, whereas NA (1 muM) had no effect. 3 In rat isolated atria pre-incubated with adrenaline and then incubated with NA, both catecholamines were taken up and were released by field stimulation. When pre-incubation was with adrenaline and incubation was with [3H]-NA, metoprolol decreased the stimulation-induced efflux of radioactivity. This effect did not occur if the atria were pre-incubated with NA instead of adrenaline, suggesting tht neuronally released adrenaline activates prejunctional beta-adrenoceptors. 4 In conscious rats, intravenously administered adrenaline (6.0 and 0.6 nmol/kg) was taken up and retained in the atria and could be released by field stimulation. The release was calcium-dependent from these rats up to 24 h after administration.
机译:1肾上腺素(10 nM)显着增强了先前与[3H]-去甲肾上腺素([3H] -NA)孵育的大鼠心房的放射性诱导的放射性外流。美托洛尔(.01μM)消除了这种作用。 2较高浓度(1μM)和NA(1μM)的肾上腺素显着降低了刺激引起的放射性外流。但是,在存在苯氧基苯甲胺(10μM)的情况下,肾上腺素(1μM)增强了流出,而NA(1μM)没有作用。 3在将大鼠肾上腺素预先与肾上腺素一起温育然后与NA一起温育的过程中,儿茶酚胺均被吸收并通过野外刺激释放。当用肾上腺素进行预孵育,用[3H] -NA进行孵育时,美托洛尔降低了刺激引起的放射性外流。如果将心房与NA而不是肾上腺素一起预孵育,则不会发生这种现象,这表明神经元释放的肾上腺素会激活结膜前β-肾上腺素受体。 4在清醒的大鼠中,静脉注射肾上腺素(6.0和0.6 nmol / kg)被吸收并保留在心房中,可以通过野外刺激释放。给药后24小时,这些大鼠的钙依赖性释放。

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