Galzi J L, Mejean A, Goeldner M, Hirth C, Ilien B
Laboratoire de Chimie Bio-Organique, C.N.R.S. (U.R.A. 1386), Faculté de Pharmacie, Université Louis Pasteur-Strasbourg, Illkirch, France.
Eur J Pharmacol. 1990 Jun 12;188(6):321-8. doi: 10.1016/0922-4106(90)90192-z.
Arylazido and aryldiazonium derivatives of carfentanil, bearing their photoactivatable function at the same position on the molecule, were synthesized. In the dark both of them exhibited similar binding affinity profiles and behaved as mu-selective and reversible ligands of the opioid receptor sites. Following irradiation, only the azido analog displayed the properties of an efficient, irreversible and selective label of the mu-opioid receptor, allowing physicochemical requirements for alkylation of this receptor subtype to be examined. Evidence is presented to consider this azido compound a promising tool for characterizing the mu-opioid receptor protein.
合成了卡芬太尼的芳基叠氮化物和芳基重氮衍生物，它们的光活化功能位于分子的同一位置。在黑暗中，它们都表现出相似的结合亲和力谱，并且作为阿片受体位点的μ选择性和可逆配体起作用。照射后，只有叠氮类似物表现出作为μ阿片受体的有效、不可逆和选择性标记的特性，从而可以研究该受体亚型烷基化的物理化学要求。有证据表明，这种叠氮化合物是表征μ阿片受体蛋白的一种有前途的工具。
