1638646-27-1

VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM[1].

VU0453379 is a highly selective CNS penetrant positive allosteric modulator of Glucagon-like peptide-1 (GLP-1) with GLP-1 EC50 = 1.3 μ,M59.2% GLP-1 max. VU0453379 potentiated low-dose exenatide to augment insulin secretion in primary mouse pancreatic islets. In a model of Parkinson′s disease it showed a significant reversal of haloperidol-induced catalepsy at 30 mg/kg.

[1] Morris LC, et al. Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM). J Med Chem. 2014 Dec 11;57(23):10192-7. DOI:10.1021/jm501375c