Synthesis of tritiated functionalized congeners of 1.3-dipropylxanthine having high affinity at adenosine receptors

✍ Scribed by Kenneth A. Jacobson; Dieter Ukena; John W. Daly; Kenneth L. Kirk

• Book ID: 102373669
• Publisher: John Wiley and Sons
• Year: 1986
• Tongue: French
• Weight: 290 KB
• Volume: 23
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.2580230509

✦ Synopsis

Two potent qgands for adenosine receptors have been synthesized with non-exchangeable 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 ,~-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.