Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl) propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): A potent, selective histamine H3 receptor inverse agonist

Journal of Medicinal Chemistry

Volumn 54, Issue 13, 2011, Pages 4781-4792

  Hudkins, Robert L ^a   Raddatz, Rita ^a   Tao, Ming ^a   Mathiasen, Joanne R ^a,f   Aimone, Lisa D ^a   Becknell, Nadine C ^a   Prouty, Catherine P ^a   Knutsen, Lars J S ^a,e   Yazdanian, Mehran ^a   Moachon, Gilbert ^b   Ator, Mark A ^a   Mallamo, John P ^a   Marino, Michael J ^a,d   Bacon, Edward R ^a   Williams, Michael ^a,c  

^a CEPHALON INC   (United States)

^b Cephalon France   (France)

^c NORTHWESTERN UNIVERSITY   (United States)

^d MERCK RESEARCH LABORATORIES   (United States)

^e Discovery Pharma Consulting LLC   (United States)

^f THOMAS JEFFERSON UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450; G PROTEIN COUPLED RECEPTOR; HISTAMINE H1 RECEPTOR; HISTAMINE H2 RECEPTOR; HISTAMINE H3 RECEPTOR; HISTAMINE H3 RECEPTOR ANTAGONIST; HISTAMINE H4 RECEPTOR; ION CHANNEL; IRDABISANT; PLASMA PROTEIN; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; ATTENTION DISTURBANCE; BINDING AFFINITY; COGNITIVE DEFECT; DRUG METABOLISM; DRUG PENETRATION; DRUG SAFETY; DRUG SOLUBILITY; EXPERIMENTAL DOG; HUMAN; LIPOPHILICITY; LIVER MICROSOME METABOLISM; MALE; MOUSE; NONHUMAN; PLASMA PROTEIN BINDING; RAT; STRUCTURE ACTIVITY RELATION; THIRST;

ANIMALS; BIOLOGICAL AVAILABILITY; BRAIN; CRYSTALLOGRAPHY, X-RAY; DOGS; DRUG INVERSE AGONISM; HISTAMINE ANTAGONISTS; HUMANS; MACACA FASCICULARIS; MALE; MICE; MICROSOMES, LIVER; PERMEABILITY; PYRIDAZINES; PYRROLIDINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, HISTAMINE H3; SOLUBILITY; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TISSUE DISTRIBUTION;

EID: 79960169443     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm200401v     Document Type: Article

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