Mutagenesis and computational docking studies support the existence of a histamine binding site at the extracellular ß3+ß3- interface of homooligomeric ß3 GABAA receptors.

Hoerbelt, Paul; Ramerstorfer, Joachim; Ernst, Margot; Sieghart, Werner; Thomson, Jeffrey L; Hough, Lindsay B; Fleck, Mark W

Hoerbelt, Paul; Ramerstorfer, Joachim; Ernst, Margot; Sieghart, Werner; Thomson, Jeffrey L; Hough, Lindsay B; Fleck, Mark W.

Afiliación

Hoerbelt P; Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, NY, 12208, USA. Electronic address: Hoerbelt@stanford.edu.
Ramerstorfer J; Department of Molecular Neurosciences, Center for Brain Research, Medical University of Vienna, Spitalgasse 4, 1090, Vienna, Austria.
Ernst M; Department of Molecular Neurosciences, Center for Brain Research, Medical University of Vienna, Spitalgasse 4, 1090, Vienna, Austria.
Sieghart W; Department of Molecular Neurosciences, Center for Brain Research, Medical University of Vienna, Spitalgasse 4, 1090, Vienna, Austria.
Thomson JL; Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, NY, 12208, USA.
Hough LB; Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, NY, 12208, USA.
Fleck MW; Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, NY, 12208, USA.

Neuropharmacology ; 108: 252-63, 2016 09.

Article en En | MEDLINE | ID: mdl-27140694

Asunto(s)

Histamina/metabolismo; Simulación del Acoplamiento Molecular/métodos; Mutagénesis/fisiología; Receptores de GABA-A/genética; Receptores de GABA-A/metabolismo; Animales; Sitios de Unión/fisiología; Relación Dosis-Respuesta a Droga; Femenino; Células HEK293; Histamina/química; Histamina/farmacología; Humanos; Estructura Secundaria de Proteína; Ratas; Receptores de GABA-A/química; Xenopus laevis

Palabras clave

(−)-bicuculline methobromide (PubChem CID: 171729); Bicuculline; Docking; GABA (PubChem CID: 119); GABA(A) receptor; Histamine; Histamine dihydrochloride (PubChem CID: 5818); Ligand-gated ion channel; Mutagenesis; Pentobarbital sodium (PubChem CID: 23676152)

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Histamina / Mutagénesis / Receptores de GABA-A / Simulación del Acoplamiento Molecular Límite: Animals / Female / Humans Idioma: En Revista: Neuropharmacology Año: 2016 Tipo del documento: Article Pais de publicación: Reino Unido

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