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

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Cha MY, Choi BC, Kang KH, Pae AN, Choi KI, Cho YS, Koh HY, Lee HY, Jung D, Kong JY

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

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

PubMed ID

11992769 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Haloperidol	Dopamine D2 receptor	Ki (nM)	18	N/A	N/A	Details
Haloperidol	Dopamine D3 receptor	Ki (nM)	25	N/A	N/A	Details