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

doi:10.1021/jm800471h

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

Research output: Contribution to journal › Article › peer-review

30 Scopus citations

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 D ₂ 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.

Original language	English (US)
Pages (from-to)	5905-5908
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	51
Issue number	19
DOIs	https://doi.org/10.1021/jm800471h
State	Published - Oct 9 2008
Externally published	Yes

ASJC Scopus subject areas

Drug Discovery
Molecular Medicine

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AU - Collins, Gregory T.

AU - Zhang, Jian

AU - Yang, Chao Yie

AU - Levant, Beth

AU - Woods, James

AU - Wang, Shaomeng

PY - 2008/10/9

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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

Abstract

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