Optimization of an ether series of mGlu5 positive allosteric modulators: Molecular determinants of MPEP-site interaction crossover

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 20, 2012, Pages 6481-6485

  Manka, Jason T ^a,b   Vinson, Paige N ^a   Gregory, Karen J ^a,e   Zhou, Ya ^a,b   Williams, Richard ^a,b   Gogi, Kiran ^a   Days, Emily ^a   Jadhav, Satya ^a   Herman, Elizabeth J ^a   Lavreysen, Hilde ^d   MacKie, Claire ^d   Bartolomé, José M ^d   MacDonald, Gregor J ^d   Steckler, Thomas ^d   Daniels, J Scott ^a,b   Weaver, C David ^a   Niswender, Colleen M ^a,b   Jones, Carrie K ^a,b,f   Conn, P Jeffrey ^a,b   Lindsley, Craig W ^a,b,c   Stauffer, Shaun R ^a,b,c   more..

^a VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b VANDERBILT UNIVERSITY MEDICAL CENTER   (United States)

^c VANDERBILT UNIVERSITY   (United States)

^d JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

^e MONASH UNIVERSITY   (Australia)

^f DEPARTMENT OF VETERANS AFFAIRS   (United States)

Author keywords

Metabotropic glutamate receptor 5; mGlu5; Non MPEP; Positive allosteric modulator (PAM)

Indexed keywords

2 METHYL 6 (PHENYLETHYNYL)PYRIDINE; AMIDE; ETHER DERIVATIVE; METABOTROPIC GLUTAMATE RECEPTOR POSITIVE ALLOSTERIC MODULATOR; METABOTROPIC RECEPTOR AGONIST; NICOTINAMIDE; UNCLASSIFIED DRUG; VU 0357121; VU 0360172; VU 0404251;

ARTICLE; CHEMICAL MODIFICATION; CHIRALITY; DRUG BINDING SITE; DRUG BRAIN LEVEL; DRUG EFFICACY; DRUG MEGADOSE; DRUG PENETRATION; DRUG POTENCY; DRUG PROTEIN BINDING; NONHUMAN; PSYCHOSIS; RAT; STRUCTURE ACTIVITY RELATION;

ALLOSTERIC REGULATION; ALLOSTERIC SITE; ANIMALS; ANTIPSYCHOTIC AGENTS; ETHERS; HUMANS; NIACINAMIDE; PSYCHOTIC DISORDERS; RATS; RECEPTORS, METABOTROPIC GLUTAMATE; STRUCTURE-ACTIVITY RELATIONSHIP;

RODENTIA;

EID: 84866742310     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.08.043     Document Type: Article

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