Abstract：
:The potential photoaffinity ligand 14-beta-(o-nitro, p-azido)-cinnamoyl-amino-N-cyclopropylmethylnormorphinone (NAM) and its derivative NOM, lacking the p-azido function, were synthesised and their opiate receptor activity determined in isolated tissue preparations. The ligands showed slow receptor kinetics. NAM was a pure competitive antagonist of met5-enkephalin responses in MVD while its antagonism of normorphine responses in GPI appeared non-competitive and non-reversible. In radioligand binding assays NOM completely and irreversibly blocked specific binding of 3H-DHM. Partial blockade of 3H-DADL specific binding was reversible by washing. No binding of NOM to kappa sites was observed. The slow receptor kinetics of NAM preclude its use as a photoaffinity ligand but suggest that a chemically more stable derivative may have a role as a pseudocovalent blocker of mu-receptors.
journal_name
Life Scijournal_title
Life sciencesauthors
Peers EM,Rance MJ,Barnard EA,Haynes AS,Smith CFdoi
10.1016/0024-3205(83)90536-2subject
Has Abstractpub_date
1983-01-01 00:00:00pages
439-42eissn
0024-3205issn
1879-0631pii
0024-3205(83)90536-2journal_volume
33 Suppl 1pub_type
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