Metabotropic glutamate receptor subtype 5 (mGlu5) and nociceptive function. I. Selective blockade of mGlu5 receptors in models of acute, persistent and chronic pain.
Neuropharmacology
; 40(1): 1-9, 2001.
Article
en En
| MEDLINE
| ID: mdl-11077065
ABSTRACT
The excitatory neurotransmitter, glutamate, is particularly important in the transmission of pain information in the nervous system through the activation of ionotropic and metabotropic glutamate receptors. A potent, subtype-selective antagonist of the metabotropic glutamate-5 (mGlu5) receptor, 2-methyl-6-(phenylethynyl)-pyridine (MPEP), has now been discovered that has effective anti-hyperalgesic effects in models of inflammatory pain. MPEP did not affect rotarod locomotor performance, or normal responses to noxious mechanical or thermal stimulation in naïve rats. However, in models of inflammatory pain, systemic administration of MPEP produced effective reversal of mechanical hyperalgesia without affecting inflammatory oedema. In contrast to the non-steroidal anti-inflammatory drugs, indomethacin and diclofenac, the maximal anti-hyperalgesic effects of orally administered MPEP were observed without acute erosion of the gastric mucosa. In contrast to its effects in models of inflammatory pain, MPEP did not produce significant reversal of mechanical hyperalgesia in a rat model of neuropathic pain.
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Base de datos:
MEDLINE
Asunto principal:
Dolor
/
Nociceptores
/
Receptores de Glutamato Metabotrópico
/
Antagonistas de Aminoácidos Excitadores
Límite:
Animals
Idioma:
En
Revista:
Neuropharmacology
Año:
2001
Tipo del documento:
Article
País de afiliación:
Suiza