| Literature DB >> 6288945 |
B E Maryanoff, E J Simon, T Gioannini, H Gorissen.
Abstract
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.Entities:
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Year: 1982 PMID： 6288945 DOI： 10.1021/jm00350a006
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446