Valenzuela R, Tachibana S, Huidobro-Toro J P
Department of Physiology, Faculty of Biological Sciences, P. Catholic University of Chile, Santiago.
Peptides. 1991 Nov-Dec;12(6):1211-4. doi: 10.1016/0196-9781(91)90196-v.
The profile of opioid activity of E-2078, a synthetic stable dynorphin analog, was examined in the mouse vas deferens bioassay and compared to that of methionine enkephalin and nonpeptide kappa agonists in the absence and in the presence of selective antagonists for the mu-, kappa- and delta-opioid receptor subtypes. The inhibitory action of E-2078 and related kappa agonists was specifically and potently antagonized only by norbinaltorphimine, revealing the presence of kappa receptors in this tissue and the predominant kappa activity of E-2078.
在小鼠输精管生物测定中检测了合成稳定强啡肽类似物E-2078的阿片样物质活性概况，并在存在和不存在μ-、κ-和δ-阿片受体亚型选择性拮抗剂的情况下，将其与甲硫氨酸脑啡肽和非肽κ激动剂的活性概况进行了比较。E-2078和相关κ激动剂的抑制作用仅被诺宾那托啡特异性且强效地拮抗，这表明该组织中存在κ受体以及E-2078具有主要的κ活性。
