Imidazo[1,2-b][1,2,4]triazines as α2/α3 subtype selective GABAA agonists for the treatment of anxiety

Autor:	George R. Marshall, Rachael Lincoln, Richard Thomas Lewis, Bindi Sohal, Susan M. Cook, Keith A. Wafford, John R. Atack, David James Hallett, Alison J. Smith, David S. Reynolds, Spencer J. Tye, Leslie J. Street, Michael G. N. Russell, Andrew Stephen Robert Jennings, Andrew Pike, José L. Castro, Joanna Stanley, Wayne F. A. Sheppard
Rok vydání:	2006
Předmět:	Male Agonist medicine.drug_class Stereochemistry Clinical Biochemistry Administration Oral Biological Availability Pharmaceutical Science Biochemistry Anxiolytic Chemical synthesis Rats Sprague-Dawley Structure-Activity Relationship Dogs Drug Discovery medicine Functional selectivity Animals GABA-A Receptor Agonists Maze Learning Receptor GABA Agonists Saimiri Molecular Biology Binding Sites Molecular Structure Bicyclic molecule Triazines GABAA receptor Chemistry Organic Chemistry Imidazoles Receptors GABA-A Anxiety Disorders In vitro Rats Disease Models Animal Protein Subunits Molecular Medicine Ataxia Female
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 16:1477-1480
ISSN:	0960-894X
Popis:	Imidazo[1,2-a]pyrimidines and imidazo[1,2-b][1,2,4]triazines are ligands for the benzodiazepine binding site of GABA(A) receptors that are functionally selective for the alpha2/alpha3 subtypes over the alpha1 subtype. SAR studies to optimise this functional selectivity, pharmacokinetic and behavioural data are described.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab2e3f49e1fb5468f2d9ea9405f453b8 https://doi.org/10.1016/j.bmcl.2005.12.044 Zobrazit plný text záznamu Full Text from ScienceDirect