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Photoaffinity ligands for the mu opioid receptor
E J Simon1, L Q Fan, J M Hiller
1Department of Psychiatry and Pharmacology, New York University Medical Center, NY 10016.
Life Sciences
|January 1, 1993
Abstract:
Two affinity ligands, 6 beta-(5-Azido-2-nitrophenacetamido) 14 beta-hydroxy-7,8-dihydromorphinone (4) and 6 beta-(5-azido-2-nitrophenacetamido) 14 beta-hydroxy-7,8-dihydro-N- cyclopropylmethylnormorphinone (5) bind reversibly to opioid receptors present in bovine caudate membranes and photolyse in a range of wavelengths centered about 366 nm to produce wash-resistant binding to the mu receptor. At these wavelengths very little if any photodestruction of the mu receptor occurs over the 20 minute period of irradiation at 0 degree C.