Centhaquin antinociception in mice is mediated by α2A- and α2B- but not α2C-adrenoceptors.
Eur J Pharmacol
; 715(1-3): 328-36, 2013 Sep 05.
Article
en En
| MEDLINE
| ID: mdl-23712005
The use of clonidine as a primary and adjuvant analgesic is well-documented. It is known that imidazoline and α2-adrenoceptors are involved in clonidine antinociception. Clonidine also produces antihypertensive actions mediated through the central nervous system. We have reported that centhaquin, a centrally-acting anti-hypertensive drug produces its hypotensive effect through a mechanism of action similar to clonidine. Centhaquin has also been shown to possess significant antinociceptive activity. Centhaquin antinociception is partially blocked by yohimbine, idazoxan, and naloxone; however, the involvement of specific adrenoceptor subtypes (α2A, α2B, or α2C) in centhaquin antinociception is unknown. The present study was conducted to determine antinociceptive properties of centhaquin citrate, a water soluble salt of centhaquin, and involvement of α2A-, α2B-, or α2C-adrenoceptors in centhaquin citrate antinociception in mice. BRL-44408 (α2A-adrenoceptor antagonist), imiloxan (α2B-adrenoceptor antagonist) and JP-1302 (α2C-adrenoceptor antagonist) were used to determine the involvement of α2A-, α2B-, or α2C-adrenoceptors, respectively. Antinociceptive (tail-flick and hot-plate) latencies were determined in male Swiss-Webster mice treated with centhaquin citrate alone and in combination with BRL-44408, imiloxan, or JP-1302. Centhaquin citrate produced significant antinociception in mice (P<0.05) which was unaffected by JP-1302 (P>0.05) but blocked by BRL-44408 (tail-flick test: 49.75% decrease, P<0.05; hot-plate test: 49.12% decrease, P<0.05) and imiloxan (tail-flick test: 46.98% decrease, P<0.05; hot-plate test: 46.42% decrease, P<0.05). This is the first report demonstrating centhaquin citrate antinociception and its blockade by BRL-44408 and imiloxan. We conclude that α2A and α2B but not α2C adrenoceptors are involved in centhaquin antinociception in mice.
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Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Piperazinas
/
Receptores Adrenérgicos alfa 2
/
Analgésicos
Límite:
Animals
Idioma:
En
Revista:
Eur J Pharmacol
Año:
2013
Tipo del documento:
Article
País de afiliación:
Estados Unidos
Pais de publicación:
Países Bajos