PubMed 21095126
Referenced in: none
Automatically associated channels: Kv11.1 , Kv8.2
Title: Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor.
Authors: Liming Shao, Jianguo Ma, Fengjiang Wang, Scott C Malcolm, Michael C Hewitt, Una C Campbell, Nancy A Spicer, Larry W Hardy, Rudy Schreiber, Kerry L Spear, Mark A Varney
Journal, date & volume: , 2010 Oct 28 , ,
PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/21095126
Abstract
The present work describes a series of novel tetrahydroquinoline amines that potently inhibit the in vitro reuptake of serotonin and dopamine (dual reuptake inhibitors). The compounds are structurally related to a series we disclosed previously, but are improved with respect to cytochrome P-450 enzyme (CYP) and potassium ion channel Kv11.1 (hERG) inhibition and synthetic accessibility. The detailed synthesis and in vitro activity and ADME profile of the compounds is described, which represent a previously undisclosed dual reuptake inhibitor chemotype.