Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABA(A)alpha2/alpha3 binding site agonists for the treatment of anxiety disorders.
J Med Chem
; 49(1): 35-8, 2006 Jan 12.
Article
em En
| MEDLINE
| ID: mdl-16392789
ABSTRACT
A series of high-affinity GABA(A) agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA(A)alpha2 and -alpha3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.
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Base de dados:
MEDLINE
Assunto principal:
Transtornos de Ansiedade
/
Pirimidinas
/
Agonistas de Receptores de GABA-A
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article