Antinociceptive effect of natural and synthetic alkamides involves TRPV1 receptors

作者：de la Rosa Lugo Vianey; Acevedo Quiroz Macdiel; Deciga Campos Myrna^*; Yolanda Rios Maria

来源：Journal of Pharmacy and Pharmacology, 2017, 69(7): 884-895.

DOI：10.1111/jphp.12721

• affinin
• alkamides
• antinociception
• capsaicin
• Heliopsis longipes

ObjectiveTo establish the role of TRPV1 receptor in the antinociceptive effect of natural alkamides (i.e. affinin, longipinamide A, longipenamide A and longipenamide B) isolated from Heliopsis longipes (A. Gray) S.F. Blake and some related synthetic alkamides (i.e. N-isobutyl-feruloylamide and N-isobutyl-dihydroferuloylamide).
MethodsThe orofacial formalin test was used to assess the antinociceptive activity of natural (1-30 g, orofacial region) and synthetic alkamides (0.1-100 g, orofacial region). The alkamide capsaicin was used as positive control, while capsazepine was used to evaluate the possible participation of TRPV1 receptor in alkamide-induced antinociception.
Key findingsNatural (1-30 g) and synthetic (0.1-100 g) alkamides administered to the orofacial region produced antinociception in mice. The antinociceptive effect induced by affinin, N-isobutyl-feruloylamide and N-isobutyl-dihydroferuloylamide was antagonized by capsazepine but not by vehicle.
ConclusionsThese results suggest that alkamide affinin, longipinamide A, longipenamide A and longipenamide B isolated from Heliopsis longipes as well as the synthesized analogue compounds N-isobutyl-feruloylamide and N-isobutyl-dihydroferuloylamide produce their effects by activating TRPV1 receptor and they may have potential for the development of new analgesic drugs for the treatment of orofacial pain.

• 出版日期2017-7