Your browser doesn't support javascript.
loading
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Goodacre, Simon C; Hallett, David J; Carling, Robert W; Castro, José L; Reynolds, David S; Pike, Andrew; Wafford, Keith A; Newman, Robert; Atack, John R; Street, Leslie J.
Afiliação
  • Goodacre SC; Neuroscience Research Centre, Merck, Sharp and Dohme Research Laboratories, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. simon.goodacre@merck.com
Bioorg Med Chem Lett ; 16(6): 1582-5, 2006 Mar 15.
Article em En | MEDLINE | ID: mdl-16384707
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones are high affinity GABA(A) agonists. Compound 16d has good oral bioavailability in rat, functional selectivity for the GABA(A)alpha2 and alpha3-subtypes and is anxiolytic in a conditioned animal model of anxiety with minimal sedation observed at full BZ binding site occupancy.
Assuntos
Buscar no Google
Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Transtornos de Ansiedade / Ansiolíticos / Agonistas GABAérgicos / Agonistas de Receptores de GABA-A Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Ano de publicação: 2006 Tipo de documento: Article
Buscar no Google
Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Transtornos de Ansiedade / Ansiolíticos / Agonistas GABAérgicos / Agonistas de Receptores de GABA-A Limite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Ano de publicação: 2006 Tipo de documento: Article