Establishing the relationship between in vitro potency, pharmacokinetic, and pharmacodynamic parameters in a series of orally available, hydroxyethylamine-derived-βsecretase inhibitors

Journal of Pharmacology and Experimental Therapeutics

Volumn 343, Issue 2, 2012, Pages 460-467

  Wood, Stephen ^a   Wen, Paul H ^a   Zhang, Jianhua ^a   Zhu, Li ^a   Luo, Yi ^a   Babu Khan, Safura ^a   Chen, Kui ^a   Pham, Roger ^a   Esmay, Joel ^a   Dineen, Thomas A ^a   Kaller, Matthew R ^a   Weiss, Matthew M ^a   Hitchcock, Stephen A ^a,b   Citron, Martin ^a,c   Zhong, Wenge ^a   Hickman, Dean ^a   Williamson, Toni ^a  

^a AMGEN INC   (United States)

^b Envoy Therapeutics   (United States)

^c UCB PHARMA   (Belgium)

Author keywords

[No Author keywords available]

Indexed keywords

AMYLOID BETA PROTEIN; BETA SECRETASE INHIBITOR; HYDROXYETHYLAMINE DERIVED BETA SECRETASE 1 INHIBITOR; MULTIDRUG RESISTANCE PROTEIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN LEVEL; CONTROLLED STUDY; DRUG ADMINISTRATION ROUTE; DRUG CLEARANCE; DRUG DESIGN; DRUG DOSE REDUCTION; DRUG METABOLISM; DRUG PENETRATION; DRUG POTENCY; DRUG STABILITY; DRUG STRUCTURE; IN VITRO STUDY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; RAT;

ADMINISTRATION, ORAL; AMYLOID BETA-PEPTIDES; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; BLOOD PROTEINS; CELL MEMBRANE PERMEABILITY; ENZYME INHIBITORS; ETHYLAMINES; FLUORESCENCE RESONANCE ENERGY TRANSFER; HEK293 CELLS; HUMANS; MALE; MICROSOMES, LIVER; P-GLYCOPROTEIN; PROTEIN BINDING; RATS; RATS, SPRAGUE-DAWLEY; RECOMBINANT PROTEINS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84867590777     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.112.197954     Document Type: Article

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