Screening of 5-HT1A receptor antagonists using molecularly imprinted polymers.
J Am Chem Soc
; 129(6): 1680-9, 2007 Feb 14.
Article
en En
| MEDLINE
| ID: mdl-17284006
ABSTRACT
Molecular imprinting produces network polymers with recognition sites for imprint molecules. The high binding affinity and selectivity in conjunction with the polymers' physical robustness positions molecular imprinted polymers (MIPs) as candidates for use as preliminary screens in drug discovery. As such, MIPs can serve as crude mimics of native receptors. In an effort to evaluate the relationship between MIPs and native receptors, imprinted polymers for WAY-100635, an antagonist of the serotonin (5-HT) receptor subtype 5-HT1A were prepared. The resulting MIP P(WAY) was evaluated as an affinity matrix in the screening of serotonin receptor antagonists with known affinities for the native receptor. Rough correlations in affinity between the synthetic P(WAY) and native receptor 5-HT1A were found. These findings provide some support for the analogy between MIPs and native receptors and their possible use as surrogates.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Piperazinas
/
Ácidos Polimetacrílicos
/
Piridinas
/
Antagonistas de la Serotonina
/
Antagonistas del Receptor de Serotonina 5-HT1
Tipo de estudio:
Diagnostic_studies
/
Prognostic_studies
/
Screening_studies
Idioma:
En
Revista:
J Am Chem Soc
Año:
2007
Tipo del documento:
Article
País de afiliación:
Estados Unidos