1207438-38-7Relevant articles and documents
Novel triple reuptake inhibitors with low risk of CAD associated liabilities: Design, synthesis and biological activities of 4-[(1S)-1-(3,4- dichlorophenyl)-2-methoxyethyl]piperidine and related compounds
Ishichi, Yuji,Kimura, Eiji,Honda, Eiji,Yoshikawa, Masato,Nakahata, Takashi,Terao, Yasuko,Suzuki, Atsuko,Kawai, Takayuki,Arakawa, Yuuichi,Ohta, Hiroyuki,Kanzaki, Naoyuki,Nakagawa, Hideyuki,Terauchi, Jun
, p. 4600 - 4613 (2013/07/26)
A novel triple reuptake inhibitor with low potential of liabilities associated with cationic amphiphilic drug (CAD) was identified following an analysis of existing drugs. Low molecular weight (MW a series of piperidine compounds was designed with consideration of the common characteristic features of CNS drugs. Optimization of the side chain by adjusting overall lipophilicity suggested that incorporation of a methoxymethyl group could provide compounds with a balance of both potent reuptake inhibition and low liability potential. Compound (S)-3a showed a potent antidepressant-like effect in the mice tail suspension test (MED = 10 mg/kg, p.o.), proportional monoamine transporter occupancies and enhancement of monoamine concentrations in mouse prefrontal cortex.