AM404 is an analog of arachidonyl ethanolamide (AEA) which potentiates the activity of endogenous AEA by blocking its re-uptake into presynaptic neurons. AM404 selectively inhibits the carrier-mediated transport of AEA without affecting anandamide hydrolysis. It inhibits the transport of AEA with an IC50 of 1 µM in rat neurons and 5 µM in rat astrocytes. In in vivo models, AM404 enhances and prolongs exogenous AEA-induced analgesia at a dose of 10 mg/kg.1
1
Beltramo, M., Stella, N., Calignano, A., et al. Functional role of high-affinity anandamide transport, as revealed by selective inhibition. Science2771094-1097(1997).
Kulkarni, P.S., and Srinivasan, B.D. Eicosapentaenoic acid metabolism in human and rabbit anterior uvea. Prostaglandins311159-1164(1986).
Beltramo, M., Stella, N., Calignano, A., et al. Functional role of high-affinity anandamide transport, as revealed by selective inhibition. Science2771094-1097(1997).
AM404 is available in the following screening
library: