| http://purl.uniprot.org/citations/30565258 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/30565258 | http://www.w3.org/2000/01/rdf-schema#comment | "Muscimol, the major psychoactive ingredient in the mushroom Amanita muscaria, has been regarded as a universal non-selective GABA-site agonist. Deletion of the GABAA receptor (GABAA R) δ subunit in mice (δKO) leads to a drastic reduction in high-affinity muscimol binding in brain sections and to a lower behavioral sensitivity to muscimol than their wild type counterparts. Here, we use forebrain and cerebellar brain homogenates from WT and δKO mice to show that deletion of the δ subunit leads to a > 50% loss of high-affinity 5 nM [3 H]muscimol-binding sites despite the relatively low abundance of δ-containing GABAA Rs (δ-GABAA R) in the brain. By subtracting residual high-affinity binding in δKO mice and measuring the slow association and dissociation rates we show that native δ-GABAA Rs in WT mice exhibit high-affinity [3 H]muscimol-binding sites (KD ~1.6 nM on α4βδ receptors in the forebrain and ~1 nM on α6βδ receptors in the cerebellum at 22°C). Co-expression of the δ subunit with α6 and β2 or β3 in recombinant (HEK 293) expression leads to the appearance of a slowly dissociating [3 H]muscimol component. In addition, we compared muscimol currents in recombinant α4β3δ and α4β3 receptors and show that δ subunit co-expression leads to highly muscimol-sensitive currents with an estimated EC50 of around 1-2 nM and slow deactivation kinetics. These data indicate that δ subunit incorporation leads to a dramatic increase in GABAA R muscimol sensitivity. We conclude that biochemical and behavioral low-dose muscimol selectivity for δ-subunit-containing receptors is a result of low nanomolar-binding affinity on δ-GABAA Rs."xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.org/dc/terms/identifier | "doi:10.1111/jnc.14646"xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/author | "Li X.G."xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/author | "Wallner M."xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/author | "Aalto A.J."xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/author | "Meera P."xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/author | "Uusi-Oukari M."xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/author | "Benkherouf A.Y."xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/author | "Soini S.L."xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/author | "Taina K.R."xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/date | "2019"xsd:gYear |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/name | "J Neurochem"xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/pages | "41-53"xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/title | "Extrasynaptic delta-GABApisub>Api/sub> receptors are high-affinity muscimol receptors."xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://purl.uniprot.org/core/volume | "149"xsd:string |
| http://purl.uniprot.org/citations/30565258 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/30565258 |
| http://purl.uniprot.org/citations/30565258 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/30565258 |
| http://purl.uniprot.org/uniprot/#_Q14AH9-mappedCitation-30565258 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/30565258 |
| http://purl.uniprot.org/uniprot/#_P22933-mappedCitation-30565258 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/30565258 |
| http://purl.uniprot.org/uniprot/#_Q8VBV6-mappedCitation-30565258 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/30565258 |
| http://purl.uniprot.org/uniprot/Q8VBV6 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/30565258 |
| http://purl.uniprot.org/uniprot/P22933 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/30565258 |
| http://purl.uniprot.org/uniprot/Q14AH9 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/30565258 |