biostudies-literatureUnknown1(8)Garbaccio RMNovel oxazolobenzimidazoles are described as potent and selective positive allosteric modulators of the metabotropic glutamate receptor 2. The discovery of this class and optimization of its physical and pharmacokinetic properties led to the identification of potent and orally bioavailable compounds (20 and 21) as advanced leads. Compound 20 (TBPCOB) was shown to have robust activity in a PCP-induced hyperlocomotion model in rat, an assay responsive to clinical antipsychotic treatments for schizophrenia.ACS medicinal chemistry letters406-10https://www.ebi.ac.uk/biostudies/studies/S-EPMC4007895biostudies-literatureDiscovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor.PMC4007895Magliaro BCFillgrove KLSmall JHGarbaccio RMHartman GDFraley METang CKuo YHutson PHUslaner JMBrnardic EJO'Brien JAJacobson MAHuszar SLfalseDiscovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor.Novel oxazolobenzimidazoles are described as potent and selective positive allosteric modulators of the metabotropic glutamate receptor 2. The discovery of this class and optimization of its physical and pharmacokinetic properties led to the identification of potent and orally bioavailable compounds (20 and 21) as advanced leads. Compound 20 (TBPCOB) was shown to have robust activity in a PCP-induced hyperlocomotion model in rat, an assay responsive to clinical antipsychotic treatments for schizophrenia.2010-01-01T00:00:00Z2010 Nov2025-04-05T10:37:28.531Z2019-03-27T01:27:30ZS-EPMC40078952490022410.1021/ml100115a