Photoaffinity ligands for the mu opioid receptor.
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.
Department of Psychiatry and Pharmacology, New York University Medical Center, NY 10016.
E J
EJ
Simon
L Q
LQ
Fan
J M
JM
Hiller
A
A
Seyed-Mozaffari
A G
AG
Schultz
S
S
Archer
D000345:Affinity Labels / Q000378:metabolism*; D000818:Animals; D001386:Azides / Q000378:metabolism*; D002417:Cattle; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008024:Ligands; D008297:Male; D009022:Morphine Derivatives / Q000378:metabolism*; D010777:Photochemistry; D017450:Receptors, Opioid, mu / Q000378:metabolism*
C083134:6-(5-azido-2-nitrophenacetamido) -14-hydroxy-7,8-dihydro-N-cyclopropylmethylmorphinone; D000345:Affinity Labels; D001386:Azides; D008024:Ligands; D009022:Morphine Derivatives; D017450:Receptors, Opioid, mu; C083133:6-(5-azido-2-nitrophenacetamido)-14-hydroxy-7,8-dihydromorphinone