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

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A piperazinylbutylisoxazole libary was designed, synthesized and screened for the binding affinities to dopamine D-2, D-3, and D-4 receptors. Several ligands were identified to possess high binding affinity and selectivity for the D-3 and D-4 receptors over the D-2 receptor. Compounds 6s and 6t showed K-i values of 2.6 nM and 3.9 nM for the D-3 receptor with 46- and 50-fold selectivity over the D-3 receptor, respectively. (C) 2002 Elsevier Science Ltd. All rights reserved.
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Issue Date
2002-05
Language
English
Article Type
Article
Keywords

MOLECULAR-CLONING; HIGH-AFFINITY; D-3 RECEPTOR; ANTAGONIST; GENE; HALOPERIDOL; EFFICACY; AGONIST; CYCLASE; POTENT

Citation

BIOORGANIC MEDICINAL CHEMISTRY LETTERS, v.12, no.10, pp.1327 - 1330

ISSN
0960-894X
URI
http://hdl.handle.net/10203/83550
Appears in Collection
CH-Journal Papers(저널논문)
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