N-arachidonoylaminophenol (AM 404) belongs to a group of bioactive N-acylamines. It is a potent activator of TRPV1 (EC50 = 26 nM), and a CB1 cannabinoid receptor ligand. Recent work on the mechanism of AM 404 has suggested that the inhibition of fatty acid amide hydrolase (FAAH) by AM 404 (IC50 = 6 μΜ) is likely responsible for all of its attributed "reuptake" properties, since intracellular FAAH hydrolysis of anandamide changes the intra/extracellular anandamide equilibrium. AM 404 also inhibits cyclooxygenase COX-1 and COX-2, thus attenuating prostaglandin synthesis. AM 404 produces analgesia in the mouse formalin and hot plate tests and potentiates the analgesic effect of anandamide in the mouse hot plate test. Furthermore, AM 404 decreases the expression of c-fos in the spinal cord of neuropathic rats, an effect inhibited by both TRPV1 and cannabinoid receptor antagonists.
产品描述
An Activator of TRPV1 Channels and a Ligand of CB1 Cannabinoid Receptors