A non-peptide NK1 receptor agonist showing subpicomolar affinity.
J Med Chem
; 47(6): 1315-8, 2004 Mar 11.
Article
en En
| MEDLINE
| ID: mdl-14998319
ABSTRACT
3-Quinolinecarboxamides have been synthesized and evaluated for their binding to the human NK(1) receptor. Several secondary amide derivatives show NK(1) receptor affinity in the picomolar range. The most active compound, hydroxymethylcarboxamide 3h showing an IC(50) value in the subpicomolar range, behaved as an agonist of NK(1) receptor in endothelial cell proliferation, inositol phosphate turnover, and NO-mediated cyclic GMP accumulation, thus proving it to be the first non-peptide NK(1) receptor agonist showing very high potency.
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Bases de datos:
MEDLINE
Asunto principal:
Quinolinas
/
Receptores de Neuroquinina-1
/
Amidas
Límite:
Animals
/
Humans
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2004
Tipo del documento:
Article
País de afiliación:
Italia