title: Design and synthesis of a piperazinylalkylisoxazole library for subtype selective dopamine receptor ligands.
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.
authors: Biochemicals Research Center, Korea Institute of Science and Technology, Cheongrayang, 130-650, Seoul, South Korea.
authors: Mi Young
authors: MY
authors: Cha
authors: Byung Chul
authors: BC
authors: Choi
authors: Kyung Ho
authors: KH
authors: Kang
authors: Ae Nim
authors: AN
authors: Pae
authors: Kung Il
authors: KI
authors: Choi
authors: Yong Seo
authors: YS
authors: Cho
authors: Hun Yeong
authors: HY
authors: Koh
authors: Hee-Yoon
authors: HY
authors: Lee
authors: Daeyoung
authors: D
authors: Jung
authors: Jae Yang
authors: JY
authors: Kong
mesh_terms: D000818:Animals; D001665:Binding Sites; D016466:CHO Cells; D003001:Cloning, Molecular; D006224:Cricetinae; D015195:Drug Design; D006801:Humans; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D007700:Kinetics; D008024:Ligands; D010879:Piperazines / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011954:Receptors, Dopamine / Q000502:physiology*; D011994:Recombinant Proteins / Q000378:metabolism; D013134:Spiperone / Q000493:pharmacokinetics; D013329:Structure-Activity Relationship; D014162:Transfection
chemical_list: D007555:Isoxazoles; D008024:Ligands; D010879:Piperazines; D011954:Receptors, Dopamine; D011994:Recombinant Proteins; D013134:Spiperone