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CJ-1639: A Potent and Highly Selective Dopamine D3 Receptor Full Agonist.

ABSTRACT: We have identified several ligands with high binding affinities to the dopamine D3 receptor and excellent selectivity over the D2 and D1 receptors. CJ-1639 (17) binds to the D3 receptor with a K(i) value of 0.50 nM and displays a selectivity of >5,000 times over D2 and D1 receptors in binding assays using dopamine receptors expressed in the native rat brain tissues. CJ-1639 binds to human D3 receptor with a K(i) value of 3.61 nM and displays over >1000-fold selectivity over human D1 and D2 receptors. CJ-1639 is active at 0.01 mg/kg at the dopamine D3 receptor in the rat and only starts to show a modest D2 activity at doses as high as 10 mg/kg. CJ-1639 is the most potent and selective D3 full agonist reported to date.

SUBMITTER: Chen J

PROVIDER: S-EPMC3224040 | biostudies-literature | 2011 Aug

REPOSITORIES: biostudies-literature

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CJ-1639: A Potent and Highly Selective Dopamine D3 Receptor Full Agonist.

Chen Jianyong J Collins Gregory T GT Levant Beth B Woods James J Deschamps Jeffrey R JR Wang Shaomeng S

ACS medicinal chemistry letters 20110801 8

We have identified several ligands with high binding affinities to the dopamine D3 receptor and excellent selectivity over the D2 and D1 receptors. CJ-1639 (17) binds to the D3 receptor with a K(i) value of 0.50 nM and displays a selectivity of >5,000 times over D2 and D1 receptors in binding assays using dopamine receptors expressed in the native rat brain tissues. CJ-1639 binds to human D3 receptor with a K(i) value of 3.61 nM and displays over >1000-fold selectivity over human D1 and D2 recep ...[more]

PMID: 22125662

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