http://purl.uniprot.org/citations/16291941 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/16291941 | http://www.w3.org/2000/01/rdf-schema#comment | "The GABA(A) receptor subtypes responsible for the anxiolytic effects of nonselective benzodiazepines (BZs) such as chlordiazepoxide (CDP) and diazepam remain controversial. Hence, molecular genetic data suggest that alpha2-rather than alpha3-containing GABA(A) receptors are responsible for the anxiolytic effects of diazepam, whereas the anxiogenic effects of an alpha3-selective inverse agonist suggest that an agonist selective for this subtype should be anxiolytic. We have extended this latter pharmacological approach to identify a compound, 4,2'-difluoro-5'-[8-fluoro-7-(1-hydroxy-1-methylethyl)imidazo[1,2-á]pyridin-3-yl]biphenyl-2-carbonitrile (TP003), that is an alpha3 subtype selective agonist that produced a robust anxiolytic-like effect in both rodent and non-human primate behavioral models of anxiety. Moreover, in mice containing a point mutation that renders alpha2-containing receptors BZ insensitive (alpha2H101R mice), TP003 as well as the nonselective agonist CDP retained efficacy in a stress-induced hyperthermia model. Together, these data show that potentiation of alpha3-containing GABA(A) receptors is sufficient to produce the anxiolytic effects of BZs and that alpha2 potentiation may not be necessary."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.org/dc/terms/identifier | "doi:10.1523/jneurosci.1166-05.2005"xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Thompson S.A."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Humphries A.C."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Atack J.R."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Reynolds D.S."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Street L.J."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Dias R."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Whiting P.J."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Rosahl T.W."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Garrett E.M."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "McKernan R.M."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Wafford K.A."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Cook S.M."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Goodacre S."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Dawson G.R."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Castro J.L."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Hallett D."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Fradley R.L."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Conley R."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Lincoln R.J."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Sheppard W.F."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Stanley J.L."xsd:string |
http://purl.uniprot.org/citations/16291941 | http://purl.uniprot.org/core/author | "Tye S.J."xsd:string |