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Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.
Abberley, Lee; Bebius, Aude; Beswick, Paul J; Billinton, Andy; Collis, Katharine L; Dean, David K; Fonfria, Elena; Gleave, Robert J; Medhurst, Stephen J; Michel, Anton D; Moses, Andrew P; Patel, Sadhana; Roman, Shilina A; Scoccitti, Tiziana; Smith, Beverley; Steadman, Jon G A; Walter, Daryl S.
Afiliação
  • Abberley L; Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom.
Bioorg Med Chem Lett ; 20(22): 6370-4, 2010 Nov 15.
Article em En | MEDLINE | ID: mdl-20934331
ABSTRACT
A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule. Compound 18 was subsequently identified as a potent P2X(7) antagonist with very low in vivo clearance and high oral bioavailability in all species examined. Some evidence to support the role of P2X(7) in the etiology of pain is also presented.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Imidazolinas / Receptores Purinérgicos P2X7 / Antagonistas Purinérgicos Tipo de estudo: Diagnostic_studies Limite: Animals Idioma: En Ano de publicação: 2010 Tipo de documento: Article
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Imidazolinas / Receptores Purinérgicos P2X7 / Antagonistas Purinérgicos Tipo de estudo: Diagnostic_studies Limite: Animals Idioma: En Ano de publicação: 2010 Tipo de documento: Article