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The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.
Wroblowski, Berthold; Wigglesworth, Mark J; Szekeres, Philip G; Smith, Graham D; Rahman, Shahzad S; Nicholson, Neville H; Muir, Alison I; Hall, Adrian; Heer, Jag P; Garland, Stephen L; Coates, William J.
Afiliação
  • Wroblowski B; GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park (North), Third Avenue, Harlow, Essex CM19 5AW, United Kingdom.
J Med Chem ; 52(3): 818-25, 2009 Feb 12.
Article em En | MEDLINE | ID: mdl-19146417
ABSTRACT
The novel 7-transmembrane receptor MrgX1 is located predominantly in the dorsal root ganglion and has consequently been implicated in the perception of pain. Here we describe the discovery and optimization of a small molecule agonist and initial docking studies of this ligand into the receptor in order to provide a suitable lead and tool compound for the elucidation of the physiological function of the receptor.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperazinas / Piridazinas / Receptores Acoplados a Proteínas G Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: J Med Chem Ano de publicação: 2009 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piperazinas / Piridazinas / Receptores Acoplados a Proteínas G Tipo de estudo: Prognostic_studies Limite: Humans Idioma: En Revista: J Med Chem Ano de publicação: 2009 Tipo de documento: Article