Actions of 3-methyl-N-oleoyldopamine, 4-methyl-N-oleoyldopamine and N-oleoylethanolamide on the rat TRPV1 receptor in vitro and in vivo

Transient Receptor Potential Channels as Drug Targets: From the Science of Basic Research to the Art of Medicine

“…On the basis of the latter finding, it was postulated that TRPV1 is an important mediator of satiety. Indeed, N-OEA, a fatty acid metabolite that suppresses appetite (see Thabuis et al, 2008;Sarro-Ramirez et al, 2013), functions as a TRPV1 agonist (Ahern, 2003;Almási et al, 2008).…”

Pharmacology of Vanilloid Transient Receptor Potential Cation Channels

“…Note the distance between the highly Ca 2ϩ -permeable TRPV5, TRPV6, and the thermoTRPs, TRPV1 to -4. (For more details, see also Yu and Catterall, 2004;Montell, 2005;Nilius et al, 2007; logs of endovanilloids, of special interest are the methylated forms of N-oleoyldopamine (3b), because reversal of activity from agonist to antagonist is observed upon O-methylation of the catechol system, with 3-methyl-N-oleoyldopamine (3c) acting as an agonist and 4-methyl-N-oleoyldopamine (3d) as an antagonist (Almá si et al, 2008). Polyamines are important endogenous regulators of TRPV1 channels that are capable of modulating inflammation and nociception.…”

TRPV1: A Potential Drug Target for Treating Various Diseases

“…N -acyl ethanolamines (NAEs), like anandamide, have been studied as activators of TRPV1. One such NAE, N -oleoylethanolamine (OLEA) (Figure 1), evokes TRPV1 currents in cells previously sensitized with protein kinase C [12]. Intraperitoneal administration of OLEA induces visceral pain behavior in wild type, but not in TRPV1-null mice [13].…”