Identification and biological characterization of 6-aryl-7-isopropylquinazolinones as novel TRPV1 antagonists that are effective in models of chronic pain.
J Med Chem
; 49(2): 471-4, 2006 Jan 26.
Article
en En
| MEDLINE
| ID: mdl-16420034
ABSTRACT
Vanilloid receptor 1 (VR1, TRPV1) is a cation-selective ion channel that is expressed on primary afferent neurons and is upregulated following inflammation and nerve damage. Blockers of this channel may have utility in the treatment of chronic nociceptive and neuropathic pain. Here, we describe the optimization from a high throughput screening hit, of a series of 6-aryl-7-isopropylquinazolinones that are TRPV1 antagonists in vitro. We also demonstrate that one compound is active in vivo against capsaicin-induced hyperalgesia and in models of neuropathic and nociceptive pain in the rat.
Search on Google
Banco de datos:
MEDLINE
Asunto principal:
Dolor
/
Quinazolinas
/
Canales Catiónicos TRPV
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
/
Humans
Idioma:
En
Año:
2006
Tipo del documento:
Article