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Bioorganic and Medicinal Chemistry Letters

Volumn 21, Issue 18, 2011, Pages 5547-5551

Impact of passive permeability and gut efflux transport on the oral bioavailability of novel series of piperidine-based renin inhibitors in rodents

(19) Lévesque, Jean Franois a Bleasby, Kelly b Chefson, Amandine a Chen, Austin a Dubé, Daniel a Ducharme, Yves a Fournier, Pierre André a Gagné, Sébastien a Gallant, Michel a Grimm, Erich a Hafey, Michael b Han, Yongxin a Houle, Robert a Lacombe, Patrick a Laliberté, Sébastien a MacDonald, Dwight a MacKay, Bruce a Papp, Robert a Tschirret Guth, Richard a

a MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH (Canada)

b MERCK RESEARCH LABORATORIES (United States)

Author keywords

Absorption; Bioavailability; Permeability; Pgp transporter; Renin

Indexed keywords

ELACRIDAR; MULTIDRUG RESISTANCE PROTEIN 1; PIPERIDINE DERIVATIVE; PYRIDONE DERIVATIVE; RENIN INHIBITOR;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG METABOLISM; DRUG PENETRATION; DRUG TRANSPORT; EXPERIMENTAL DOG; INTESTINE ABSORPTION; LIPOPHILICITY; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PASSIVE TRANSPORT; RAT; STRUCTURE ACTIVITY RELATION; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ANIMALS; BIOLOGICAL AVAILABILITY; BIOLOGICAL TRANSPORT; CELL MEMBRANE PERMEABILITY; DOSE-RESPONSE RELATIONSHIP, DRUG; MICE; MICE, KNOCKOUT; MOLECULAR STRUCTURE; P-GLYCOPROTEINS; PIPERIDINES; RATS; RENIN; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS; RODENTIA;

EID: 80051933539 PISSN: 0960894X EISSN: 14643405 Source Type: Journal
DOI: 10.1016/j.bmcl.2011.06.095 Document Type: Article

Times cited : (12)

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