94308-84-6Relevant academic research and scientific papers
Hybrid approach for the design of highly affine and selective dopamine D3 receptor ligands using privileged scaffolds of biogenic amine GPCR ligands
Sasse, Britta C.,Mach, Ulrich R.,Leppaenen, Jukka,Calmels, Thierry,Stark, Holger
, p. 7258 - 7273 (2008/03/27)
A series of compounds containing privileged scaffolds of the known histamine H1 receptor antagonists cetirizine, mianserin, ketotifen, loratadine, and bamipine were synthesized for further optimization as ligands for the related biogenic amine binding dopamine D3 receptor. A pharmacological screening was carried out at dopamine D2 and D3 receptors. In the preliminary testing various ligands have shown moderate to high affinities for dopamine D3receptors, for example, N-(4-{4-[benzyl(phenyl)amino]piperidin-1-yl}butylnaphthalen-2-carboxamide (19a) (hD3 Ki = 0.3 nM; hD2 Ki = 703 nM), leading to a selectivity ratio of 2343.
Synthesis and in vitro and in vivo functional studies of Ortho- substituted phenylpiperazine and N-substituted 4-N-(o- methoxyphenyl)aminopiperidine analogues of WAY100635
Mensonides-Harsema, Marguérite M.,Liao, Yi,B?ttcher, Henning,Bartoszyk, Gerd D.,Greiner, Hartmunt E.,Harting, Jürgen,De Boer, Peter,Wikstr?m, H?kan V.
, p. 432 - 439 (2007/10/03)
WAY100635 (2), N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2- pyridinyl)cyclohexane-carboxamide, is a silent serotonin 5-HT(1A) antagonist, which is now widely used to study the 5-HT(1A) receptor both in vivo and in vitro. In this paper, we describe
