ARN272 (ARN-272) is a specific, competitive FAAH-like anandamide transporter (FLAT) inhibitor, antagonizes [3H]-anandamide binding to purified FLAT (IC50=1.8 uM) and inhibits [3H]-anandamide accumulation in FLAT-expressing HEK293 cells with IC50 of 3 uM.
ARN272 (1 mg/kg intraperitoneal, i.p.) in mice increased plasma levels of anandamide without changing the levels of 2-AG, OEA or PE.
ARN272 produces CB1-dependent antinociception, attenuates nociceptive and inflammatory pain in mice.
ARN272 tonically activates CB1 receptors and as such produces a type of indirect agonism to regulate toxin-induced nausea and vomiting.
FAAH-like anandamide transporter (FLAT) is a partly cytosolic variant of the intracellular anandamide-degrading enzyme, fatty acid amide hydrolase-1 (FAAH-1).
FLAT was proposed to function as an intracellular AEA carrier and mediate its delivery to FAAH for hydrolysis. Pharmacological inhibition of FLAT potentiated AEA signaling and produced antinociceptive effects.