N-(1,2-diphenylethyl)piperazines: a new class of dual serotonin/noradrenaline reuptake inhibitor.
The synthesis and structure-activity relationships of a novel series of piperazine derivatives as dual inhibitors of serotonin and noradrenaline reuptake is described. Two compounds possessed comparable in vitro profiles to the dual reuptake inhibitor duloxetine.
Jonathan Fray
M
M
Sandwich Chemistry, Pfizer Global Research and Development, Sandwich, UK. jonathan.fray@pfizer.com
Bish
Gerwyn
G
Brown
Alan D
AD
Fish
Paul V
PV
Stobie
Alan
A
Wakenhut
Florian
F
Whitlock
Gavin A
GA
D000588:Amines / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D000068736:Duloxetine Hydrochloride; D006801:Humans; D008956:Models, Chemical; D009638:Norepinephrine / Q000737:chemistry*; D010879:Piperazines / Q000737:chemistry*; D012701:Serotonin / Q000737:chemistry*; D050486:Serotonin Plasma Membrane Transport Proteins / Q000737:chemistry; D017367:Selective Serotonin Reuptake Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000494:pharmacology
D000588:Amines; D000068736:Duloxetine Hydrochloride; D009638:Norepinephrine; D010879:Piperazines; D012701:Serotonin; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors; D013876:Thiophenes