REVISTA

La hemopresina, un agonista inverso de los receptores de cannabinoides, inhibe el dolor neuropático en ratas

Descripción: La hemopresina (Hp) se une selectivamente a los receptores cannabinoides CB1 (receptores CB1) y ejerce una acción antinociceptiva en los modelos de dolor inflamatorio. Se demuestra que Hp muestra antinocicepción en el dolor de etiología neuropática

TITULO FUENTE ORIGINAL:

Hemopressin, an inverse agonist of cannabinoid receptors, inhibits neuropathic pain in rats

AUTORES:

Toniolo EF, Maique ET, Ferreira WA Jr, Heimann AS, Ferro ES, Ramos-Ortolaza DL, Miller L, Devi LA, Dale CS

REVISTA ABREV.:

Peptides

AÑO:

2020

REFERENCIA:

56:125-31

DOI:

10.1016/j.peptides.2014.03.016

RESUMEN ORIGINAL:

Direct-acting cannabinoid receptor ligands are well known to reduce hyperalgesic responses after nerve injury, although their psychoactive side effects have damped enthusiasm for their therapeutic development. Hemopressin (Hp) is a nonapeptide that selectively binds CB1 cannabinoid receptors (CB1 receptors) and exerts antinociceptive action in inflammatory pain models. We investigated the... + Leer más

Direct-acting cannabinoid receptor ligands are well known to reduce hyperalgesic responses after nerve injury, although their psychoactive side effects have damped enthusiasm for their therapeutic development. Hemopressin (Hp) is a nonapeptide that selectively binds CB1 cannabinoid receptors (CB1 receptors) and exerts antinociceptive action in inflammatory pain models. We investigated the effect of Hp on neuropathic pain in rats subjected to chronic constriction injury (CCI) of the sciatic nerve, and explored the mechanisms involved. Oral administration of Hp inhibits mechanical hyperalgesia of CCI-rats up to 6h. Hp treatment also decreases Egr-1 immunoreactivity (Egr-1Ir) in the superficial layer of the dorsal horn of the spinal cord of CCI rats. The antinociceptive effect of Hp seems to be independent of inhibitory descending pain pathway since methysergide (5HT1A receptor antagonist) and yohimbine (α-2 adrenergic receptor antagonist) were unable to prevent Hp antinociceptive effect. Hp decreased calcium flux on DRG neurons from CCI rats, similarly to that observed for AM251, a CB1 receptor antagonist. We also investigated the effect of Hp on potassium channels of CCI rats using UCL 1684 (a blocker of Ca(2+)-activated K(+) channels) which reversed Hp-induced antinociception. Furthermore, concomitant administration of URB-584 (FAAH inhibitor) but not JZL-184 (MAGL inhibitor) potentiates antinociceptive effect of Hp in CCI rats indicating an involvement of anadamide on HP-induced antinociception. Together, these data demonstrate that Hp displays antinociception in pain from neuropathic etiology through local effects. The release of anandamide and the opening of peripheral K(+) channels are involved in the antinociceptive effect

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Enlace al pdf de acceso libre: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC[...]