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Recent progress in the discovery of niacin receptor agonists.
Semple, Graeme; Boatman, P Douglas; Richman, Jeremy G.
Afiliação
  • Semple G; Arena Pharmaceuticals Inc, 6166 Nancy Ridge Drive, San Diego, CA 92127, USA. gsemple@arenapharm.com
Curr Opin Drug Discov Devel ; 10(4): 452-9, 2007 Jul.
Article em En | MEDLINE | ID: mdl-17659487
Niacin (nicotinic acid) favorably affects multiple serum lipid parameters that are believed to be cardiovascular risk factors, but is also associated with a cutaneous flushing adverse effect. The recent discovery of a G-protein-coupled receptor target for niacin (termed GPR109alpha) has stimulated interest in the discovery of new compounds with niacin-like effects on lipids, but with fewer adverse effects. This review discusses the progress made toward the discovery of such molecules and highlights the pharmacological models used to enable their identification. The advances made in both these areas may help to determine whether GPR109alpha is the molecular target responsible for the beneficial anti-atherogenic effects of niacin.
Assuntos
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Receptores Acoplados a Proteínas G / Niacina Tipo de estudo: Prognostic_studies / Risk_factors_studies Limite: Animals Idioma: En Ano de publicação: 2007 Tipo de documento: Article
Buscar no Google
Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Receptores Acoplados a Proteínas G / Niacina Tipo de estudo: Prognostic_studies / Risk_factors_studies Limite: Animals Idioma: En Ano de publicação: 2007 Tipo de documento: Article