Potential affinity labels for the opiate receptor based on fentanyl and related compounds
作者:Bruce E. Maryanoff、Eric J. Simon、Theresa Gioannini、H. Gorissen
DOI:10.1021/jm00350a006
日期:1982.8
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.