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Your search keyword '"Wang, Fengjiang"' showing total 2 results
Start Over Author "Wang, Fengjiang" Topic dopamine uptake inhibitors
2 results on '"Wang, Fengjiang"'

1. Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor.

Author

Shao L, Hewitt MC, Wang F, Malcolm SC, Ma J, Campbell JE, Campbell UC, Engel SR, Spicer NA, Hardy LW, Schreiber R, Spear KL, and Varney MA

Subjects
Amines chemistry, Amines pharmacology, Animals, Antidepressive Agents chemical synthesis, Antidepressive Agents chemistry, Antidepressive Agents pharmacology, Cyclization, Inhibitory Concentration 50, Methane chemistry, Methane pharmacology, Mice, Molecular Structure, Rats, Stereoisomerism, Amines chemical synthesis, Dopamine Uptake Inhibitors chemical synthesis, Dopamine Uptake Inhibitors chemistry, Dopamine Uptake Inhibitors pharmacology, Drug Design, Methane chemical synthesis, Norepinephrine chemical synthesis, Norepinephrine chemistry, Norepinephrine pharmacology, Serotonin chemical synthesis, Serotonin chemistry, Serotonin pharmacology
Abstract

The current work discloses a novel cyclohexylarylamine chemotype with potent inhibition of the serotonin, norepinephrine, and dopamine transporters and potential for treatment of major depressive disorder. Optimized compounds 1 (SERT, NET, DAT, IC(50)=169, 85, 21 nM) and 42 (SERT, NET, DAT IC(50)=34, 295, 90 nM) were highly brain penetrant, active in vivo in the mouse tail suspension test at 30 mpk po and were not general motor stimulants., (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Published
2011
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2. Discovery of 1-(3,4-dichlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydroquinolin-4-amine, a dual serotonin and dopamine reuptake inhibitor.

Author

Shao L, Ma J, Wang F, Malcolm SC, Hewitt MC, Campbell UC, Spicer NA, Hardy LW, Schreiber R, Spear KL, and Varney MA

Subjects
Animals, Dopamine Plasma Membrane Transport Proteins metabolism, Dopamine Uptake Inhibitors chemical synthesis, Dopamine Uptake Inhibitors pharmacokinetics, Drug Evaluation, Preclinical, Humans, Mice, Microsomes metabolism, Quinolines chemical synthesis, Quinolines pharmacokinetics, Serotonin Plasma Membrane Transport Proteins metabolism, Selective Serotonin Reuptake Inhibitors chemical synthesis, Selective Serotonin Reuptake Inhibitors pharmacokinetics, Dopamine Plasma Membrane Transport Proteins antagonists & inhibitors, Dopamine Uptake Inhibitors chemistry, Quinolines chemistry, Serotonin Plasma Membrane Transport Proteins chemistry, Selective Serotonin Reuptake Inhibitors chemistry
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., (Copyright © 2010 Elsevier Ltd. All rights reserved.)

Published
2011
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