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研究阿片受体的特殊困难在于,受体的量很少(10fmol/mg 豚鼠脑)而且是膜结合的蛋白质,对蛋白水解酶和去垢剂敏感。一项有前途的研究是应用亲和标记,特别是光亲和标记技术。然而,目前已证明使用短波长(254nm)的紫外光能使阿片受体的结合活性迅速破坏。鉴此,作者设计并合成了一个分子中含有在长波长处具有足够的最大吸收发色团的阿片受体光亲和标记试剂〔D-丙~2,亮~5〕-脑啡肽N-〔(2-硝基-4-叠氮苯)氨基]乙胺(ENAPE)。本文报道ENAPE 的合成、生物
A special difficulty with opioid receptors is that the amount of receptor is small (10 fmol / mg guinea pig brain) and is a membrane-bound protein that is sensitive to proteolytic enzymes and detergents. A promising study is the use of affinity tags, especially photoaffinity labeling. However, it has now been demonstrated that the use of short wavelength (254 nm) UV light can rapidly destroy the binding activity of opioid receptors. In view of this, the authors designed and synthesized an opioid receptor photoaffinity labeling reagent [D-Prop-2, BrdU-5] having an absorption maximal number of chromophores at a long wavelength in its molecule, enkephalin N- [ (2-nitro-4-azidobenzene) amino] ethylamine (ENAPE). This article reports the synthesis of ENAPE, biology