Multiparameter optimization in CNS drug discovery: Design of pyrimido[4,5-d]azepines as potent 5-hydroxytryptamine 2C (5-HT2C) receptor agonists with exquisite functional selectivity over 5-HT2A and 5-HT2B receptors

Journal of Medicinal Chemistry

Volumn 57, Issue 12, 2014, Pages 5258-5269

  Storer, R Ian ^a   Brennan, Paul E ^a,d   Brown, Alan D ^a   Bungay, Peter J ^a   Conlon, Kelly M ^a   Corbett, Matthew S ^b   Depianta, Robert P ^b   Fish, Paul V ^a,e   Heifetz, Alexander ^c   Ho, Danny K H ^a   Jessiman, Alan S ^a   McMurray, Gordon ^a   De Oliveira, Cesar Augusto F ^a   Roberts, Lee R ^a   Root, James A ^a   Shanmugasundaram, Veerabahu ^b   Shapiro, Michael J ^b   Skerten, Melanie ^a   Westbrook, Dominique ^a   Wheeler, Simon ^a   Whitlock, Gavin A ^a   Wright, John ^a   more..

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

^b PFIZER INC   (United States)

^c EVOTEC UK LTD   (United Kingdom)

^d UNIVERSITY OF OXFORD   (United Kingdom)

^e UNIVERSITY OF LONDON   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2 BENZYL 9 METHYL 4 (METHYLAMINO) 5,6,8,9 TETRAHYDRO 7H PYRIMIDO[4,5 D]AZEPINE; 2 [DIFLUORO(PHENYL)METHYL] N METHYL 6,7,8,9 TETRAHYDRO 5H PYRIMIDO[4,5 D]AZEPIN 4 AMINE; 5 HYDROXYTRYPTAMINE 2C RECEPTOR AGONIST; AZEPINE DERIVATIVE; CENTRAL NERVOUS SYSTEM AGENTS; G PROTEIN COUPLED RECEPTOR; LORCASERIN; PF 4479745; PF 4522654; PYRIMIDINE DERIVATIVE; PYRIMIDO[4,5 D]AZEPINE DERIVATIVE; SEROTONIN 2A RECEPTOR; SEROTONIN 2B RECEPTOR; SEROTONIN AGONIST; UNCLASSIFIED DRUG; VABICASERIN;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DOG; DRUG EFFICACY; DRUG PENETRATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; DRUG TARGETING; FEMALE; HUMAN; HUMAN CELL; HUMAN TISSUE; MOLECULAR MODEL; NONHUMAN; STRESS INCONTINENCE; STRUCTURE ACTIVITY RELATION;

ANIMALS; AZEPINES; BLOOD-BRAIN BARRIER; CENTRAL NERVOUS SYSTEM AGENTS; CHO CELLS; CRICETULUS; DOGS; DRUG DESIGN; HUMANS; MADIN DARBY CANINE KIDNEY CELLS; PERMEABILITY; PYRIMIDINES; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTOR, SEROTONIN, 5-HT2B; RECEPTOR, SEROTONIN, 5-HT2C; SEROTONIN 5-HT2 RECEPTOR AGONISTS; STRUCTURE-ACTIVITY RELATIONSHIP; URINARY INCONTINENCE, STRESS;

EID: 84903535031     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm5003292     Document Type: Article

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