Discovery of (S)-2-cyclopentyl- N -((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1 H-pyrrido[3,4-b ]indole-4-carboxamide (VU0453379): A novel, cns penetrant glucagon-like peptide 1 receptor (glp-1r) positive allosteric modulator (PAM)

Journal of Medicinal Chemistry

Volumn 57, Issue 23, 2014, Pages 10192-10197

  Morris, Lindsey C ^a   Nance, Kellie D ^b,c   Gentry, Patrick R ^b   Days, Emily L ^b   Weaver, C David ^b   Niswender, Colleen M ^b   Thompson, Analisa D ^b   Jones, Carrie K ^b   Locuson, Chuck W ^b   Morrison, Ryan D ^b   Daniels, J Scott ^b   Niswender, Kevin D ^a,c   Lindsley, Craig W ^b,c  

^a VANDERBILT UNIVERSITY MEDICAL CENTER   (United States)

^b VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

^c VANDERBILT UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 CYCLOPENTYL N (1 ISOPROPYLPYRROLIDIN2 YL) 9 METHYL 1 OXO 2,9 DIHYDRO 1H PYRRIDO[3,4 B]INDOLE 4 CARBOXAMIDE; EXENDIN 4; GLUCAGON LIKE PEPTIDE 1 RECEPTOR AGONIST; UNCLASSIFIED DRUG; (S)-2-CYCLOPENTYL-N-((1-ISOPROPYLPYRROLIDIN2-YL)-9-METHYL-1-OXO-2,9-DIHYDRO-1H-PYRRIDO(3,4-B)INDOLE-4-CARBOXAMIDE; CENTRAL NERVOUS SYSTEM AGENTS; GLP1R PROTEIN, MOUSE; GLUCAGON LIKE PEPTIDE 1; GLUCAGON LIKE PEPTIDE 1 RECEPTOR; GLUCAGON RECEPTOR; HALOPERIDOL; INDOLE DERIVATIVE; INSULIN; PEPTIDE; PYRROLIDINE DERIVATIVE; VENOM;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; DRUG METABOLISM; DRUG SYNTHESIS; HALOPERIDOL-INDUCED CATALEPSY; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; HUMAN TISSUE; INSULIN RELEASE; LOW DRUG DOSE; MALE; MOUSE; NONHUMAN; PANCREAS ISLET; RAT; TIME TO MAXIMUM PLASMA CONCENTRATION; VOLUME OF DISTRIBUTION; ALLOSTERISM; ANIMAL; C57BL MOUSE; CATALEPSY; CHEMICALLY INDUCED; DRUG EFFECTS; DRUG POTENTIATION; LIVER MICROSOME; METABOLISM; SECRETION (PROCESS); STRUCTURE ACTIVITY RELATION; SYNTHESIS;

ALLOSTERIC REGULATION; ANIMALS; CATALEPSY; CENTRAL NERVOUS SYSTEM AGENTS; DRUG SYNERGISM; GLUCAGON-LIKE PEPTIDE 1; GLUCAGON-LIKE PEPTIDE-1 RECEPTOR; HALOPERIDOL; HIGH-THROUGHPUT SCREENING ASSAYS; INDOLES; INSULIN; ISLETS OF LANGERHANS; MALE; MICE, INBRED C57BL; MICROSOMES, LIVER; PEPTIDES; PYRROLIDINES; RECEPTORS, GLUCAGON; STRUCTURE-ACTIVITY RELATIONSHIP; VENOMS;

EID: 84918528163     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501375c     Document Type: Article

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