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Tritium labelling of enkephalin analogs : Tyr‐D‐Ala‐Gly‐NH‐CH(CH 3 )‐CH 2 ‐CH(CH 3 ) 2 (trimu 4), Tyr‐D‐Ser‐Gly‐Phe‐Leu‐Thr (DSLET), Tyr‐D‐Thr‐Gly‐Phe‐Leu‐Thr (DTLET), μ and δ opiate‐receptors specific ligands
Author(s) -
Gacel G.,
Dodey P.,
Roques B. P.,
Morgat J. L.,
Roy J.,
Fromageot P.
Publication year - 1983
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580200606
Subject(s) - chemistry , enkephalin , tritium , labelling , stereochemistry , chemical synthesis , receptor , biochemistry , in vitro , opioid , physics , nuclear physics
Unambiguous biochemical characterization of the different opiate receptors (i.e., μ and δ) imperatively requires fully specific and radiolabelled ligands. Therefore, in this paper, we report the synthesis of the 3,5‐dibromotyrosyl precursors of three highly selective peptides : Tyr‐D‐Ala‐Gly‐NH‐CH(CH 3 )‐CH 2 ‐CH(CH 3 ) 2 , TRIMU 4 (μ) Tyr‐D‐Ser‐Gly‐Phe‐Leu‐Thr, DSLET (δ) and Tyr‐D‐Thr‐Gly‐Phe‐Leu‐Thr, DTLET (δ). Reductive tritiation by exchange with 3 H 2 leads to the labelled enkephalins analogs in high yields and with specific activities between 45 to 60 Ci/mmole.