457627-11-1Relevant articles and documents
Design and Synthesis of a Piperazinylalkylisoxazole Library for Subtype Selective Dopamine Receptor Ligands
Cha, Mi Young,Choi, Byung Chul,Kang, Kyung Ho,Pae, Ae Nim,Choi, Kung Il,Cho, Yong Seo,Koh, Hun Yeong,Lee, Hee-Yon,Jung, Daeyoung,Kong, Jae Yang
, p. 1327 - 1330 (2002)
A piperazinylbutylisoxazole library 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 Ki values of 2.6 nM and 3.9 nM for the D3 receptor with 46- and 50-fold selectivity over te D2 receptor, respectively.