PMID: 9416772Jan 1, 1997Paper

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

Life Sciences
M D'AmicoF Rossi

Abstract

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.

References

Feb 15, 1991·Biochemical Pharmacology·M R Boarder, D B Marriott
Jan 1, 1991·Life Sciences·R B RaffaH I Jacoby
May 24, 1994·Proceedings of the National Academy of Sciences of the United States of America·K IshikawaT Nagase

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Citations

Mar 28, 2017·Neuropeptides·Rachel Feldman-Goriachnik, Menachem Hanani
Jun 19, 2002·Cardiovascular Drug Reviews·Megumu Okada, Masaru Nishikibe
Nov 5, 2020·Experimental Brain Research·Luís Alexandre LombaAleksander Roberto Zampronio

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