期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 17, 页码 5612-5617出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.07.003
关键词
Dopamine 3 receptor; Full agonists; Structure-activity-relationships
资金
- National Institute on Drug Abuse, National Institutes of Health [R01DA020669]
- NIDA, NIH [NIDA Y1-DA-0101-02]
We have designed, synthesized and evaluated a series of new compounds with the goal to identify potent and selective D-3 ligands. The two most potent and selective new D-3 ligands are compounds 38 and 52, which bind to the D-3 receptors with a K-i value of <1 nM and display a selectivity of 450-494 times over the D-2 receptors and >10,000 times over the D-1 receptors. Both 38 and 52 are full agonists with high potency at the D-3 receptor in a D-3 functional assay. (C) 2012 Elsevier Ltd. All rights reserved.
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