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The use of [ 3 H]‐[ d ‐Pen 2 , d ‐Pen 5 ]enkephalin as a highly selective ligand for the δ‐binding site
Author(s) -
Cotton R.,
Kosterlitz H.W.,
Paterson S.J.,
Rance M.J.,
Traynor J.R.
Publication year - 1985
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1985.tb17387.x
Subject(s) - enkephalin , chemistry , guinea pig , stereochemistry , binding site , binding affinities , affinities , endocrinology , medicine , biochemistry , receptor , opioid , biology
1 The characteristics of the binding of [ 3 H]‐[ d ‐Pen 2 , d ‐Pen 5 ]enkephalin were determined in homogenates of guinea‐pig and rat brain. 2 In the guinea‐pig, the maximum binding capacity for [ 3 H]‐[ d ‐Pen 2 , d ‐Pen 5 ]enkephalin was 4.19 pmol g −1 and the K D 1.61 n m . In the rat, the corresponding values were 2.47 pmol g −1 and 5.42 n m . In both species, the maximum binding capacity and the affinity were not altered when μ‐binding was suppressed with [ d ‐Ala 2 , MePhe 4 , Gly‐ol 5 ]enkephalin. 3 The μ‐agonists, [ d ‐Ala 2 , MePhe 4 , Gly‐ol 5 ]enkephalin and morphine, displaced a small portion of the binding of [ 3 H]‐[ d ‐Pen 2 , d ‐Pen 5 ]enkephalin with high affinities.