Kinetic and system bias as drivers of metabotropic glutamate receptor 5 allosteric modulator pharmacology.

Sengmany, Kathy; Hellyer, Shane D; Albold, Sabine; Wang, Taide; Conn, P Jeffrey; May, Lauren T; Christopoulos, Arthur; Leach, Katie; Gregory, Karen J

Sengmany, Kathy; Hellyer, Shane D; Albold, Sabine; Wang, Taide; Conn, P Jeffrey; May, Lauren T; Christopoulos, Arthur; Leach, Katie; Gregory, Karen J.

Afiliação

Sengmany K; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Department of Pharmacology, Monash University, Parkville, VIC, Australia.
Hellyer SD; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Department of Pharmacology, Monash University, Parkville, VIC, Australia.
Albold S; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Department of Pharmacology, Monash University, Parkville, VIC, Australia.
Wang T; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Department of Pharmacology, Monash University, Parkville, VIC, Australia.
Conn PJ; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN, USA.
May LT; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Department of Pharmacology, Monash University, Parkville, VIC, Australia.
Christopoulos A; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Department of Pharmacology, Monash University, Parkville, VIC, Australia.
Leach K; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Department of Pharmacology, Monash University, Parkville, VIC, Australia.
Gregory KJ; Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Department of Pharmacology, Monash University, Parkville, VIC, Australia. Electronic address: karen.gregory@monash.edu.

Neuropharmacology ; 149: 83-96, 2019 05 01.

Article em En | MEDLINE | ID: mdl-30763654

Assuntos

Regulação Alostérica/efeitos dos fármacos; Ligantes; Receptor de Glutamato Metabotrópico 5/metabolismo; Animais; Cálcio/metabolismo; Sistema Nervoso Central; Feminino; Células HEK293; Humanos; Fosfatos de Inositol/metabolismo; Cinética; Camundongos; Gravidez; Cultura Primária de Células; Ratos

Palavras-chave

(PubChem CID: 108001); (PubChem CID: 16036762); (PubChem CID: 162834); (PubChem CID: 3025961); (PubChem CID: 44557636); (PubChem CID: 57328392); (PubChem CID: 9794218); (l-glutamic acid PubChem CID: 33032); Biased modulation; DHPG; Glutamate; Kinetics; M-5MPEP; MPEP; MTEP; Metabotropic glutamate receptor 5; Negative allosteric modulator; VU0366058; dipraglurant; fenobam

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Regulação Alostérica / Receptor de Glutamato Metabotrópico 5 / Ligantes Tipo de estudo: Prognostic_studies Limite: Animals / Female / Humans / Pregnancy Idioma: En Ano de publicação: 2019 Tipo de documento: Article

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