Bach-Dieterle Y, Holden W E, Junod A F
Br J Pharmacol. 1983 Dec;80(4):603-11. doi: 10.1111/j.1476-5381.1983.tb10049.x.
We studied the muscle relaxation induced by adenine and several adenine derivatives in strips of tracheal smooth muscle from pigs; in addition their metabolism by the tissue was examined. Adenine relaxed tissue which was contracted by carbachol, histamine, or KCl. Adenine's potency was similar to that of adenosine and ATP (threshold about 4 X 10(-5)M). In tissues with carbachol-induced tone, the adenine effect differed from adenosine and ATP by being slower in onset and in 'washout' time. Furthermore, neither dipyridamole nor theophylline modified the response to adenine. The relationship was examined between pharmacological effects and the metabolism of [3H]-adenosine and [3H]-adenine. Both substrates were taken up by the tissue and converted to nucleotides, but relaxation correlated with nucleotide accumulation only in the case of [3H]-adenine. We conclude that the site and mechanism of adenine-induced relaxation is different from that of adenosine and ATP in porcine tracheal muscle.
我们研究了腺嘌呤及几种腺嘌呤衍生物对猪气管平滑肌条的肌肉松弛作用;此外,还检测了这些物质在组织中的代谢情况。腺嘌呤可使由卡巴胆碱、组胺或氯化钾引起收缩的组织松弛。腺嘌呤的效力与腺苷和三磷酸腺苷相似(阈值约为4×10⁻⁵M)。在有卡巴胆碱诱导张力的组织中,腺嘌呤的作用在起效时间和“洗脱”时间方面与腺苷和三磷酸腺苷不同,起效较慢。此外,双嘧达莫和茶碱均未改变对腺嘌呤的反应。研究了[³H] - 腺苷和[³H] - 腺嘌呤的药理作用与代谢之间的关系。两种底物均被组织摄取并转化为核苷酸,但仅在[³H] - 腺嘌呤的情况下,松弛作用与核苷酸积累相关。我们得出结论,在猪气管肌肉中,腺嘌呤诱导松弛的部位和机制与腺苷和三磷酸腺苷不同。