Description
AM-404 (198022-70-7) inhibits anandamide transport (IC50?= 1 μM) without inhibiting anandamide amidase or activating cannabinoid receptors.1,2?Vanilloid receptors are activated by AM-404.3?Active?in vivo.1
Biological Activity
Competitive and selective inhibitor of carrier-mediated anandamide transport (IC 50 = 1 μ M). Does not activate CB 1 receptors or inhibit anandamide hydrolysis but has been shown to activate native and cloned vanilloid receptors (pEC 50 = 7.4). Active in vivo . Also available in water soluble emulsion (N-(4-Hydroxyphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide ).
References
1) Calignano?et al. (1997),?Potentiation of anandamide hypotension by the transport inhibitor AM404; Eur. J. Pharmacol.,?337?R1
2) Beltramo?et al. (1997), Functional role of high-affinity anandamide transport, as revealed by selective inhibition; Science,?277?1094
3) Zygmunt?et al. (2000),?The anandamide inhibitor AM404 activates vanilloid receptors: Eur. J. Pharmacol.?396?39
