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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Selective and non-selective ET antagonists reveal an ET(A)/ET(B) receptor mediated ET-1-induced antinociceptive effect in PAG area of mice.

The injection of endothelin-1 (ET-1) (2 pmol) into the dorsolateral periaqueductal gray area (PAG) of mice produces antinociceptive effect as underscored by increases in the latency time for the reaction to a hot plate. Pretreatment of the PAG area with bosentan (10 nmol) (a mixed ET(A)/ET(B) receptor antagonist), FR 139317 (5 nmol) (ET[A] receptor selective antagonist) or BQ-788 (5 nmol) (ET[B] receptor selective antagonist) greatly reduced the antinociceptive effect induced by ET-1. Therefore, ET-1 induces antinociceptive effects via both ET(A)/ET(B) receptors. In addition, since ET-antagonists lowered per se the control reaction time of the mice when administered alone to the PAG area, we would suggest that endogenous ET-1 acting within the PAG area contributes to the suppression of pain.[1]

References

  1. Selective and non-selective ET antagonists reveal an ET(A)/ET(B) receptor mediated ET-1-induced antinociceptive effect in PAG area of mice. D'Amico, M., Di Filippo, C., Rossi, F. Life Sci. (1997) [Pubmed]
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