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Design, Synthesis, and Evaluation of Potent and Selective Ligands for the Dopamine 3 (D3) Receptor With a Novel in Vivo Behavioral Profile

Jianyong Chen, Gregory T Collins, Jian Zhang, Chao-Yie Yang, Beth Levant, James Woods, Shaomeng Wang

J Med Chem. 2008 Oct 9;51(19):5905-8.

PMID: 18785726

Abstract:

A series of compounds structurally related to pramipexole were designed, synthesized, and evaluated as ligands for the dopamine 3 (D3) receptor. Compound 12 has a K(i) value of 0.41 nM to D3 and a selectivity of >30000- and 800-fold over the D1-like and D2 receptors, respectively. Our in vivo functional assays showed that this compound is a partial agonist at the D3 receptor with no detectable activity at the D2 receptor.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP106092095 Pramipexole Related Compound A Pramipexole Related Compound A 106092-09-5 Price
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