Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.
J Med Chem
; 45(26): 5710-20, 2002 Dec 19.
Article
em En
| MEDLINE
| ID: mdl-12477354
ABSTRACT
The synthesis and binding study of new 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide 3-ester compounds are reported. A pharmacological evaluation of the high-affinity ligands 1-4 belonging to the 3-heteroarylester series is made. The 3-(2-thienylmethoxycarbonyl) derivative 4 stands out from the other heteroarylesters and is found, using nine different behavioral methods, to be a functionally selective ligand in vivo it shows anxiolytic-like activity in the conflict models (light-dark box and plus maze test) similarly to diazepam, without any sedative and amnesic properties or interference from alcohol.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ansiolíticos
/
Triazinas
/
Receptores de GABA-A
/
GABAérgicos
/
Óxidos N-Cíclicos
/
Compostos Heterocíclicos com 3 Anéis
Tipo de estudo:
Etiology_studies
Idioma:
En
Revista:
J Med Chem
Ano de publicação:
2002
Tipo de documento:
Article