Rónai A Z, Berzétei I P, Kurgyis J
Institute for Drug Research, Budapest, Hungary.
Cell Mol Neurobiol. 1981 Dec;1(4):335-42. doi: 10.1007/BF00716268.
The inhibitory effects of various opiates on developing rat vas deferens were studied by determining the degree of depression of mechanical responses elicited by electrical field stimulation. All agonists showed decreased effects with maturation, but the decrease occurred at different times. With normorphine the loss of agonist activity was greatest at days 12-16, while with D-Met2,Pro5-enkephalinamide it was greatest at days 16-30. beta-Endorphin also was less effective in adult than 30-day preparations, but methionine enkephalin was ineffective at all ages. Morphine and normorphine were weak antagonists of opiate agonists in the adult preparations. These results indicate that the nature and pharmacologic sensitivity of opiate actions change with development.
通过测定电场刺激引发的机械反应的抑制程度，研究了各种阿片类药物对发育中的大鼠输精管的抑制作用。所有激动剂的作用随成熟而降低，但降低发生在不同时间。对于去甲吗啡，激动剂活性在第12 - 16天损失最大，而对于D - Met2，Pro5 - 脑啡肽酰胺，在第16 - 30天损失最大。β-内啡肽在成年制剂中也比30天的制剂效果差，但甲硫氨酸脑啡肽在所有年龄段均无效。吗啡和去甲吗啡在成年制剂中是阿片类激动剂的弱拮抗剂。这些结果表明，阿片类药物作用的性质和药理敏感性随发育而变化。
