Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators

Autor:	Dana E. Rodriguez, Jean-Michel Vernier, Hutchinson John H, Hervé Schaffhauser, Anthony B. Pinkerton, Lorrie P. Daggett, Joyce K. James, Michael F. Gardner, Blake A. Rowe, Una Campbell, Rowena V. Cube
Rok vydání:	2005
Předmět:	Clinical Biochemistry Pharmaceutical Science Pharmacology Receptors Metabotropic Glutamate Biochemistry Structure-Activity Relationship Allosteric Regulation Drug Discovery Animals Molecular Biology Molecular Structure Metabotropic glutamate receptor 5 Chemistry Metabotropic glutamate receptor 4 Organic Chemistry Metabotropic glutamate receptor 7 Metabotropic glutamate receptor 6 Brain Potentiator Rats Disease Models Animal Metabotropic receptor Models Chemical Indans Schizophrenia Molecular Medicine Metabotropic glutamate receptor 1 Metabotropic glutamate receptor 2 Protein Binding
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 15:1565-1571
ISSN:	0960-894X
Popis:	We have identified and synthesized a series of phenyl-tetrazolyl and 4-thiopyridyl indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation, as well as PK properties, led to the discovery of 28 (EC50 = 186 nM), which displayed activity in a rodent model for schizophrenia.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8e1edf523edbd2b8328be76da134078 https://doi.org/10.1016/j.bmcl.2005.01.077 Zobrazit plný text záznamu Full Text from ScienceDirect