307952-37-0Relevant academic research and scientific papers
Construction of a cis-Cyclopropane via Reductive Radical Decarboxylation. Enantioselective Synthesis of cis- and trans-1-Arylpiperazyl-2-phenylcyclopropanes Designed as Antidopaminergic Agents
Yamaguchi, Kazuya,Kazuta, Yuji,Abe, Hiroshi,Matsuda, Akira,Shuto, Satoshi
, p. 9255 - 9262 (2007/10/03)
(1S,2S)-, (1S,2R)-, and (1R,2S)-1-(2,4-Dimethylphenyl)piperazyl-2-phenylcyclopropane (2a, 3, and ent-3, respectively), which were designed as conformationally restricted analogues of haloperidol (1), a clinically effective antipsychotic agent, were synthe
trans-1-[(2-phenylcyclopropyl)methyl]-4-arylpiperazines: Mixed dopamine D2/D4 receptor antagonists as potential antipsychotic agents
Zhang,Hodgetts,Rachwal,Zhao,Wasley,Craven,Brodbeck,Kieltyka,Hoffman,Bacolod,Girard,Tran,Thurkauf
, p. 3923 - 3932 (2007/10/03)
The dopaminergic receptor profile of a series of trans-1-[(2-phenylcyclopropyl)methyl]-4-arylpiperazines was examined. Aromatic substitution patterns were varied with the goal of identifying a compound having affinities for the D2 and D4 receptors in a ratio similar to that observed for the atypical neuroleptic clozapine. The compounds (1S,2S)-trans-1-[(2-phenylcyclopropyl)methyl]-4-(2,4-dichlorophenyl)piperazin e (5m) and (1S,2S)-trans-1-[(2-phenylcyclopropyl)methyl]-4-(2,4-dimethylphenyl)piperazin e (5t) were selected for functional antagonists at D2 and D4 receptors and had a D2/D4 ratio approximating that of clozapine; they proved inactive in behavioral tests of antipsychotic activity.
