Dibenzazecine scaffold rebuilding--is the flexibility always essential for high dopamine receptor affinities?
Bioorg Med Chem
; 17(19): 6898-907, 2009 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-19744859
ABSTRACT
The moderately flexible 7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecines are known to be potent dopamine receptor antagonists, whereas the corresponding rigid dibenzo[d,g]quinolizines are inactive. We built the scaffolds of dibenzo[c,g], [c,f] and [d,f]azecines and together with their ring closed, more rigid precursors, evaluated the affinities for the human D(1)-D(5) receptors (radioligand binding) as well as the functionalities (calcium assay) and thus investigated the influence of annelation and conformative flexibility of these compounds on their affinity for human cloned dopamine receptors.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Quinolizinas
/
Receptores Dopaminérgicos
/
Antagonistas de Dopamina
/
Compostos Heterocíclicos
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2009
Tipo de documento:
Article
País de afiliação:
Alemanha