Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands
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
- Appears in Collection
- CH-Journal Papers(저널논문)
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