131899-86-0

Upstream product

• 2627-86-3 (S)-1-phenyl-ethylamine 
• 939-90-2 trans-2-phenylcyclopropane-1-carboxylic acid 
• 23020-15-7 (1S,2S)-2-phenylcyclopropane-1-carboxylic acid 
• 939-87-7 (1SR,2SR)-2-phenylcyclopropanecarbonyl chloride 

Downstream Products

• 307952-37-0 [4-(2,4-Dimethyl-phenyl)-piperazin-1-yl]-((1S,2S)-2-phenyl-cyclopropyl)-methanone 
• 307952-30-3 [4-(2,4-Dichloro-phenyl)-piperazin-1-yl]-((1S,2S)-2-phenyl-cyclopropyl)-methanone 
• 23020-15-7 (1S,2S)-2-phenylcyclopropane-1-carboxylic acid 

Relevant academic research and scientific papers

Discovery and optimization of Lu AF58801, a novel, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors: Attenuation of subchronic phencyclidine (PCP)-induced cognitive deficits in rats following oral administration

In this Letter, we describe a chemical lead optimization campaign starting from a novel, weak α7 nicotinic acetylcholine receptor positive allosteric modulator (PAM) hit from a HTS screen. Exploration of the structure-activity relationships for α7 PAM potency, intrinsic hepatic clearance, the structure-property relationships for lipophilicity, and thermodynamic solubility, led to the identification of Lu AF58801: a potent, orally available, brain penetrant PAM of the α7 nicotinic acetylcholine receptor, showing efficacy in a novel object recognition task in rats treated subchronically with phencyclidine (PCP).

trans-1-[(2-phenylcyclopropyl)methyl]-4-arylpiperazines: Mixed dopamine D2/D4 receptor antagonists as potential antipsychotic agents

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.