Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: Design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence

Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 9, 2011, Pages 2715-2720

  Andrews, Mark D ^a   Fish, Paul V ^a   Blagg, Julian ^a   Brabham, Tiffini K ^a   Brennan, Paul E ^a   Bridgeland, Alison ^a   Brown, Alan D ^a   Bungay, Peter J ^a   Conlon, Kelly M ^a   Edmunds, Nicholas J ^a   Af Forselles, Kerry ^a   Gibbons, Colleen P ^b   Green, Martin P ^a   Hanton, Giles ^a   Holbrook, Mark ^a   Jessiman, Alan S ^a   McIntosh, Karin ^a   McMurray, Gordon ^a   Nichols, Carly L ^a   Root, James A ^a   Storer, R Ian ^a   Sutton, Michael R ^a   Ward, Robin V ^a   Westbrook, Dominique ^a   Whitlock, Gavin A ^a   more..

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^b PFIZER INC   (United States)

Author keywords

5 HT2C receptor agonists; PF 3246799; Pyrimido 4,5 d azepines; Urinary incontinence

Indexed keywords

LORCASERIN; PF 3246799; PYRIMIDO[4,5 D]AZEPINE; SEROTONIN 2A RECEPTOR; SEROTONIN 2B RECEPTOR; SEROTONIN 2C AGONIST; UNCLASSIFIED DRUG; VABICASERIN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; AREA UNDER THE CURVE; CONFERENCE PAPER; DOG; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PLASMA CLEARANCE; RAT; STRESS INCONTINENCE; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; AZEPINES; DISEASE MODELS, ANIMAL; DOGS; MALE; MOLECULAR STRUCTURE; PYRIMIDINES; RATS; SEROTONIN 5-HT2 RECEPTOR AGONISTS; URINARY INCONTINENCE;

EID: 79955468385     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.11.120     Document Type: Conference Paper

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