Pyridyl-phenyl ether monoamine reuptake inhibitors: Impact of lipophilicity on dual SNRI pharmacology and off-target promiscuity

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 9, 2008, Pages 2896-2899

  Whitlock, Gavin A ^a   Fish, Paul V ^a   Fray, M Jonathan ^a   Stobie, Alan ^a   Wakenhut, Florian ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

5 HT reuptake; Lipophilicity; NA reuptake; Off target promiscuity; Polypharmacology; Pyridyl phenyl ether

Indexed keywords

PYRIDYLPHENYL ETHER MONOAMINE REUPTAKE INHIBITOR; SEROTONIN NORADRENALIN REUPTAKE INHIBITOR;

ALKYLATION; AMINATION; ARTICLE; DOPAMINE RECEPTOR BLOCKING; DRUG SELECTIVITY; DRUG STRUCTURE; HUMAN; HUMAN CELL; IN VITRO STUDY; LIPOPHILICITY; NEUROPHARMACOLOGY; REDUCTION; STRUCTURE ACTIVITY RELATION;

AMINES; HEPATOCYTES; HUMANS; INHIBITORY CONCENTRATION 50; MODELS, CHEMICAL; NOREPINEPHRINE; PHENYL ETHERS; PYRIDINES; RECEPTOR, SEROTONIN, 5-HT1A; SEROTONIN UPTAKE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 42949142178     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.03.082     Document Type: Article

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22. i < 1000 nM. This result reinforced the hypothesis that lipophilicity was the main contributor to the promiscuous nature of examples 13, 16 and 21.