TY - JOUR
T1 - Antinociceptive effect of natural and synthetic alkamides involves TRPV1 receptors
AU - de la Rosa-Lugo, Vianey
AU - Acevedo-Quiroz, Macdiel
AU - Déciga-Campos, Myrna
AU - Rios, María Yolanda
N1 - Publisher Copyright:
© 2017 Royal Pharmaceutical Society
PY - 2017/7/1
Y1 - 2017/7/1
N2 - Objective: To 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). Methods: The orofacial formalin test was used to assess the antinociceptive activity of natural (1–30 μg, orofacial region) and synthetic alkamides (0.1–100 μg, 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 findings: Natural (1–30 μg) and synthetic (0.1–100 μg) 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. Conclusions: These 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.
AB - Objective: To 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). Methods: The orofacial formalin test was used to assess the antinociceptive activity of natural (1–30 μg, orofacial region) and synthetic alkamides (0.1–100 μg, 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 findings: Natural (1–30 μg) and synthetic (0.1–100 μg) 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. Conclusions: These 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.
KW - Heliopsis longipes
KW - affinin
KW - alkamides
KW - antinociception
KW - capsaicin
UR - http://www.scopus.com/inward/record.url?scp=85017363976&partnerID=8YFLogxK
U2 - 10.1111/jphp.12721
DO - 10.1111/jphp.12721
M3 - Artículo
C2 - 28374409
SN - 0022-3573
VL - 69
SP - 884
EP - 895
JO - Journal of Pharmacy and Pharmacology
JF - Journal of Pharmacy and Pharmacology
IS - 7
ER -