140465-79-8Relevant academic research and scientific papers
Design, synthesis, and evaluation of hexahydrobenz[f]isoquinolines as a novel class of dopamine 3 receptor ligands
Wu, Xihan,Chen, Jianyong,Ji, Min,Varady, Judith,Levant, Beth,Wang, Shaomeng
, p. 5813 - 5816 (2004)
We previously identified hexahydrobenz[f]isoquinoline (4a) as a new class of dopamine 3 receptor (D3) ligand. Herein, we described the design, synthesis, and preliminary structure-activity relationships of new analogues of 4a as a novel class of D3 ligands. Among these new analogues, compound 4h is a potent D3 ligand (Ki = 6.1 nM) and has a selectivity of 133-fold between D3- and D2-like receptors, and of 163-fold between D3- and D1-like receptors, respectively. Thus, compound 4h represents a promising new lead compound for further design and optimization toward achieving highly potent and selective D3 ligands.
Benzisoquinoline Analogues as High-Affinity ? Ligands
Russell, Michael G. N.,Baker, Raymond,Billington, David C.,Knight, Antony K.,Middlemiss, Derek N.,Noble, Alison J.
, p. 2025 - 2033 (2007/10/02)
This paper describes the synthesis of some conformationally restricted 4-phenylpiperidine analogues and their affinities for the guinea pig cerebellum ? recognition site (-DTG) and the rat striatum dopamine D2 receptor (-(-)-sulpiride)
