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A CONFORMATIONAL ANALYSIS FOR LEUCINE‐ENKEPHALIN USING ACTIVITY AND BINDING DATA OF SYNTHETIC ANALOGUES
Author(s) -
BEDDELL C.R.,
CLARK R.B.,
LOWE L.A.,
WILKINSON S.,
CHANG K.J.,
CUATRECASAS P.,
MILLER R.
Publication year - 1977
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.1476-5381.1977.tb08427.x
Subject(s) - leucine , enkephalin , chemistry , biochemistry , stereochemistry , amino acid , receptor , opioid
1 Leucine‐enkephalin and some analogues were assayed for activity in vitro on the mouse vas deferens and for binding to opiate receptors from rat brain. 2 The experimental data were analysed in terms of the stringency for glycine, a D‐amino acid or an L‐amino acid at each position in the peptide. 3 The observed configurational specificity was compared with the stringency that would be predicted to occur if enkephalin adopted certain hydrogen‐bonded conformations at the receptor. 4 A small subset of the conformations examined was found to be compatible with the experimental data.