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Synthesis of tritiated functionalized congeners of 1.3‐dipropylxanthine having high affinity at adenosine receptors
Author(s) -
Jacobson Kenneth A.,
Ukena Dieter,
Daly John W.,
Kirk Kenneth L.
Publication year - 1986
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.2580230509
Subject(s) - chemistry , adenosine , congener , stereochemistry , receptor , selectivity , potency , chemical synthesis , adenosine receptor , catalysis , biochemistry , agonist , in vitro , organic chemistry
Two potent ligands for adenosine receptors have been synthesized with non‐exchangeable 3 H labeling to high specific activity. Both are adenosine antagonists. one a carboxylic acid congener, 1 , and the other an amino congener. 2 . and are structurally related to 1,3‐dipropyl‐8‐phenylxanthine. The label was introduced at four positions in the n‐propyl groups through catalytic reduction of 1,3‐diallyl precursors. Due to favorable aqueous solubility. high potency and selectivity. these ligands are expected to be suitable for competitive binding assays and autoradiography.