Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator

Autor:	Andreas Ritzen, Christoffer Bundgaard, Robbin Brodbeck, Rikke Sindet, Nannette Svendsen, Morten Hentzer
Rok vydání:	2009
Předmět:	Allosteric modulator Receptor Metabotropic Glutamate 5 Clinical Biochemistry Allosteric regulation Administration Oral Pharmaceutical Science Pharmacology Receptors Metabotropic Glutamate Biochemistry Mice Structure-Activity Relationship chemistry.chemical_compound Allosteric Regulation Heterocyclic Compounds In vivo mental disorders Drug Discovery Animals Potency Molecular Biology Metabotropic glutamate receptor 5 Organic Chemistry Brain Biological activity Rats chemistry Alkynes Molecular Medicine Penetrant (biochemical) Lead compound
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 19:3275-3278
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2009.04.095
Popis:	This Letter describes the discovery of a novel series of mGluR5 positive allosteric modulators (PAMs). The lead compound, 11c, exhibits excellent potency (EC(50)=30 nM) in vitro, and reaches high brain levels in both rats and mice after oral administration.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::203a7eedf537646a5221f2061fac8287 https://doi.org/10.1016/j.bmcl.2009.04.095 Zobrazit plný text záznamu Full Text from ScienceDirect