Work

Discovery of Oxazolobenzimidazoles as Positive Allosteric Modulators for the mGluR2 Receptor

Year: 2010

Type: article

Abstract: 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.

Source: ACS Medicinal Chemistry Letters

DOI: 10.1021/ml100115a

Authors: Robert M. Garbaccio, Edward J. Brnardic, Mark E. Fraley, George D. Hartman, Pete H. Hutson, Julie A. O'Brien, Brian C. Magliaro, Jason M. Uslaner, Sarah L. Huszar, Kerry L. Fillgrove, James H. Small, Cuyue Tang, Yuhsin Kuo, Marlene A. Jacobson

Institution: Institute for In Vitro Sciences

Language: English

Topic: Neuroscience and Neuropharmacology Research

Subfield: Cellular and Molecular Neuroscience

Field: Neuroscience

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: green

OpenAlex ID: W2051144559

FWCI: 1.544

Cites: 24

Cited by: 22

Related to: 10