μ阿片受体的光亲和配体。
Photoaffinity ligands for the mu opioid receptor.
作者信息
Simon E J, Fan L Q, Hiller J M, Seyed-Mozaffari A, Schultz A G, Archer S
机构信息
Department of Psychiatry and Pharmacology, New York University Medical Center, NY 10016.
出版信息
Life Sci. 1993;53(14):1173-8. doi: 10.1016/0024-3205(93)90554-g.
Two affinity ligands, 6 beta-(5-Azido-2-nitrophenacetamido) 14 beta-hydroxy-7,8-dihydromorphinone (4) and 6 beta-(5-azido-2-nitrophenacetamido) 14 beta-hydroxy-7,8-dihydro-N- cyclopropylmethylnormorphinone (5) bind reversibly to opioid receptors present in bovine caudate membranes and photolyse in a range of wavelengths centered about 366 nm to produce wash-resistant binding to the mu receptor. At these wavelengths very little if any photodestruction of the mu receptor occurs over the 20 minute period of irradiation at 0 degree C.
两种亲和配体，6β-(5-叠氮基-2-硝基苯乙酰胺基)-14β-羟基-7,8-二氢吗啡酮(4)和6β-(5-叠氮基-2-硝基苯乙酰胺基)-14β-羟基-7,8-二氢-N-环丙基甲基去甲吗啡酮(5)与牛尾状核膜中存在的阿片受体可逆结合，并在以366nm为中心的一系列波长下光解，从而产生对μ受体的耐洗结合。在这些波长下，在0℃照射20分钟的时间内，μ受体几乎没有发生光破坏（如果有也是极少的）。
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