Description
VU0453379 is an allosteric agonist and positive allosteric modulator (ago-PAM) of glucagon-like peptide 1 receptor (GLP-1R).1 It induces calcium mobilization in 9-3-H cells expressing human GLP-1R (EC50 = 1.3 µM) and enhances GLP-1-, exenatide-, or liraglutide-induced calcium mobilization in the same cells (EC50s = 1.8, 8.4, and 30 µM, respectively). VU0453379 (30 µM) potentiates exenatide-induced insulin secretion in primary mouse pancreatic islets. It reverses catalepsy induced by haloperidol (Item No. 12014) in a rat model of Parkinson’s disease motor symptoms when administered at a dose of 30 mg/kg.WARNING This product is not for human or veterinary use.
References
[1] LINDSEY C. MORRIS. 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]. Journal of Medicinal Chemistry, 2014, 57 23: 10192-10197. DOI:
10.1021/jm501375c
