Maryanoff B E, Simon E J, Gioannini T, Gorissen H
J Med Chem. 1982 Aug;25(8):913-9. doi: 10.1021/jm00350a006.
Derivatives of fentanyl, 3-methylfentanyl, sufentanil, and lofentanil, possessing chemo- or photoaffinity functionalities, were synthesized as potential affinity reagents for the opiate receptor. Opiate receptor binding constants (IC50) were determined in competition experiments with [3H]naloxone and [3H]naltrexone. Affinity-labeling experiments were generally unsuccessful, although some irreversible attachment was achieved with alpha-diazoamide 17 and aryl azide 23.
合成了具有化学或光亲和功能的芬太尼、3-甲基芬太尼、舒芬太尼和洛芬太尼的衍生物，作为阿片受体的潜在亲和试剂。在与[3H]纳洛酮和[3H]纳曲酮的竞争实验中测定了阿片受体结合常数（IC50）。尽管用α-重氮酰胺17和芳基叠氮化物23实现了一些不可逆的结合，但亲和标记实验总体上并不成功。
