期刊
JOURNAL OF PHARMACY AND PHARMACOLOGY
卷 69, 期 7, 页码 884-895出版社
WILEY
DOI: 10.1111/jphp.12721
关键词
affinin; alkamides; antinociception; capsaicin; Heliopsis longipes
资金
- Conacyt, Mexico [241044]
- UAEM-Mexico (PIDE) [PII02, PICA18]
- ESM-IPN [SIP: 20170861]
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.
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