Hybrid approach for the design of highly affine and selective dopamine D(3) receptor ligands using privileged scaffolds of biogenic amine GPCR ligands.
Bioorg Med Chem
; 15(23): 7258-73, 2007 Dec 01.
Article
em En
| MEDLINE
| ID: mdl-17826096
ABSTRACT
A series of compounds containing privileged scaffolds of the known histamine H(1) receptor antagonists cetirizine, mianserin, ketotifen, loratadine, and bamipine were synthesized for further optimization as ligands for the related biogenic amine binding dopamine D(3) receptor. A pharmacological screening was carried out at dopamine D(2) and D(3) receptors. In the preliminary testing various ligands have shown moderate to high affinities for dopamine D(3)receptors, for example, N-(4-{4-[benzyl(phenyl)amino]piperidin-1-yl}butylnaphthalen-2-carboxamide (19a) (hD(3)K(i)=0.3 nM; hD(2)K(i)=703 nM), leading to a selectivity ratio of 2343.
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Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
/
Receptores de Dopamina D3
/
Antagonistas dos Receptores Histamínicos H1
Idioma:
En
Revista:
Bioorg Med Chem
Ano de publicação:
2007
Tipo de documento:
Article
País de afiliação:
Alemanha