A Novel &#945;2/&#945;4 Subtype-selective Positive Allosteric Modulator of Nicotinic Acetylcholine Receptors Acting from the C-tail of an &#945; Subunit.

Wang, Jingyi; Kuryatov, Alexander; Jin, Zhuang; Norleans, Jack; Kamenecka, Theodore M; Kenny, Paul J; Lindstrom, Jon

A Novel α2/α4 Subtype-selective Positive Allosteric Modulator of Nicotinic Acetylcholine Receptors Acting from the C-tail of an α Subunit.

Wang, Jingyi; Kuryatov, Alexander; Jin, Zhuang; Norleans, Jack; Kamenecka, Theodore M; Kenny, Paul J; Lindstrom, Jon.

Afiliação

Wang J; From the Department of Neuroscience, Perelman School of Medicine at the University of Pennsylvania, Philadelphia, Pennsylvania 19104.
Kuryatov A; From the Department of Neuroscience, Perelman School of Medicine at the University of Pennsylvania, Philadelphia, Pennsylvania 19104.
Jin Z; Department of Molecular Therapeutics, Scripps Research Institute, Scripps, Florida 33458, and.
Norleans J; From the Department of Neuroscience, Perelman School of Medicine at the University of Pennsylvania, Philadelphia, Pennsylvania 19104.
Kamenecka TM; Department of Molecular Therapeutics, Scripps Research Institute, Scripps, Florida 33458, and.
Kenny PJ; Department of Pharmacology and Systems Therapeutics, Icahn School of Medicine at Mount Sinai, New York, New York 10029.
Lindstrom J; From the Department of Neuroscience, Perelman School of Medicine at the University of Pennsylvania, Philadelphia, Pennsylvania 19104, JSLKK@mail.med.upenn.edu.

J Biol Chem ; 290(48): 28834-46, 2015 Nov 27.

Article em En | MEDLINE | ID: mdl-26432642

Assuntos

Imidazóis; Agonistas Nicotínicos; Receptores Nicotínicos/metabolismo; Regulação Alostérica/efeitos dos fármacos; Regulação Alostérica/fisiologia; Estradiol/metabolismo; Células HEK293; Humanos; Imidazóis/química; Imidazóis/farmacocinética; Imidazóis/farmacologia; Agonistas Nicotínicos/química; Agonistas Nicotínicos/farmacocinética; Agonistas Nicotínicos/farmacologia; Estrutura Terciária de Proteína; Receptores Nicotínicos/genética

Palavras-chave

drug development; electrophysiology; nicotine addition; nicotinic acetylcholine receptors (nAChR); positive allosteric modulator; receptor desensitization; receptor structure-function

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Receptores Nicotínicos / Agonistas Nicotínicos / Imidazóis Limite: Humans Idioma: En Revista: J Biol Chem Ano de publicação: 2015 Tipo de documento: Article País de publicação: Estados Unidos

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