3,4-Dihydro-2H-benzoxazinones are 5-HT1A receptor antagonists with potent 5-HT reuptake inhibitory activity

Bioorganic and Medicinal Chemistry Letters

Volumn 15, Issue 3, 2005, Pages 737-741

  Atkinson, Peter J ^a   Bromidge, Steven M ^a   Duxon, Mark S ^a   Gaster, Laramie M ^a   Hadley, Michael S ^a   Hammond, Beverley ^a   Johnson, Christopher N ^a   Middlemiss, Derek N ^a   North, Stephanie E ^a   Price, Gary W ^a   Rami, Harshad K ^a   Riley, Graham J ^a   Scott, Claire M ^a   Shaw, Tracey E ^a   Starr, Kathryn R ^a   Stemp, Geoffrey ^a   Thewlis, Kevin M ^a   Thomas, David R ^a   Thompson, Mervyn ^a   Vong, Antonio K K ^a   Watson, Jeannette M ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

BENZOXAZINONE DERIVATIVE; SEROTONIN; SEROTONIN 1A ANTAGONIST; SEROTONIN 1A RECEPTOR; SEROTONIN 1B RECEPTOR; SEROTONIN 1D RECEPTOR;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BINDING SITE; BRAIN; CONTROLLED STUDY; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG PENETRATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SCREENING; HUMAN; HUMAN CELL; INHIBITION KINETICS; NONHUMAN; RAT;

ANIMALS; BENZOXAZINES; BIOLOGICAL AVAILABILITY; BRAIN; CELL LINE; DRUG STABILITY; HUMANS; RADIOLIGAND ASSAY; RATS; RECEPTOR, SEROTONIN, 5-HT1A; SEROTONIN UPTAKE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP; SYNAPTOSOMES;

EID: 19944433806     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.11.030     Document Type: Article

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14. Prepared from the corresponding phenol by treatment with excess 1,2-dibromoethane and potassium carbonate in 2-butanone at reflux
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17. HPLC method: Chiralpak AD, 50/50/0.1 hexane/ethanol/triethylamine
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