Berdysheva L V, Boĭko O V, Manukhin B N
Izv Akad Nauk Ser Biol. 2009 Nov-Dec(6):714-20.
The effect of cocaine (10 microM) on the kinetics of contractile response to noradrenaline (NA) was studied in the rat epididymal and prostatic vas deferens. Cocaine caused an acute increase in vas deferens adrenergic sensitivity primarily due to blockage of NA neuronal capture. The presynaptic action prevailed in the epididymal half: the EC50 value decreased 32-fold with a slight increase of the maximum adrenergic response more evident in the prostatic half. In the presence of cocaine, the prostatic contraction to NA was mediated not by a single pool of alpha1-adrenoceptors like in epididymal vas deferens but by two. Its high affinity pool had the same affinity as alpha1-adrenoceptors of the epididymal half, the affinity value of the low one was 36-fold less, and the total maximal response of both pools increased 4.5-fold. The differences in cocaine effect on the rat epididymal and prostatic vas deferens contractions to NA appear to be caused by the different sources of Ca2+ involved in these responses.
在大鼠附睾和前列腺输精管中研究了可卡因(10微摩尔)对去甲肾上腺素(NA)收缩反应动力学的影响。可卡因导致输精管肾上腺素能敏感性急性增加,主要是由于NA神经元摄取受阻。突触前作用在附睾段占主导:半数有效浓度(EC50)值降低了32倍,最大肾上腺素能反应略有增加,在前列腺段更明显。在有可卡因存在的情况下,前列腺对NA的收缩不是像附睾输精管那样由单一的α1肾上腺素能受体池介导,而是由两个受体池介导。其高亲和力受体池与附睾段的α1肾上腺素能受体具有相同的亲和力,低亲和力受体池的亲和力值小36倍,两个受体池的总最大反应增加了4.5倍。可卡因对大鼠附睾和前列腺输精管对NA收缩作用的差异似乎是由这些反应中涉及的不同钙源引起的。