Premium
Probes for narcotic receptor mediated phenomena 8. Tritiation of irreversible mu or delta specific opioid receptor affinity ligands to high specific activity
Author(s) -
Burke Terrence R.,
Rice Kenner C.,
Jacobson Arthur E.,
Simonds William F.,
Klee Werner A.
Publication year - 1984
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.2580210802
Subject(s) - chemistry , tritium , ligand (biochemistry) , amine gas treating , μ opioid receptor , opioid receptor , opioid , tritium illumination , receptor , δ opioid receptor , specific activity , narcotic antagonists , stereochemistry , combinatorial chemistry , organic chemistry , biochemistry , (+) naloxone , enzyme , physics , nuclear physics
Abstract Tritiation of the delta‐specific opioid alkylating ligand FIT, 3 and the mu‐specific opioid alkylating ligand BIT, 9 to high specific activity is described. Both compounds were derived from dibrominated amino intermediates ( 4 and 10 , respectively) which were tritiated with tritium gas over Pd/C before conversion of the amine functions to isothiocyanates.