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Bioorg Med Chem Lett. 2002 May 20;12(10):1327-30.

Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.

Author information

1
Biochemicals Research Center, Korea Institute of Science and Technology, Cheongrayang, 130-650, Seoul, South Korea.

Abstract

A piperazinylbutylisoxazole libary was designed, synthesized and screened for the binding affinities to dopamine D2, D3, and D4 receptors. Several ligands were identified to possess high binding affinity and selectivity for the D3 and D4 receptors over the D2 receptor. Compounds 6s and 6t showed K(i) values of 2.6 nM and 3.9 nM for the D3 receptor with 46- and 50-fold selectivity over the D2 receptor, respectively.

PMID:
11992769
DOI:
10.1016/s0960-894x(02)00179-8
[Indexed for MEDLINE]

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