UCM707

Numerous analogs of arachidonoyl ethanolamide (AEA, anandamide) potentiate its biological activity.¹ This potentiation is ascribed either to inhibition of AEA reuptake into neurons, or inhibition of fatty acid amide hydrolase (FAAH) within the neurons.² One of the more potent and selective reuptake inhibitors is UCM707, a 3-furyl arachidonoyl analog. UCM707 has an IC₅₀ of 0.8 µM for the inhibition of tritiated AEA uptake into human U937 cells but has low affinity for FAAH, exhibiting an IC₅₀ value of 30 µM.³ UCM707 also potentiates the biological effects of AEA when co-administered in rats.⁴

WARNING This product is not for human or veterinary use.

1. Devane, W.A., Hanus, L., Breuer, A., et al. Isolation and structure of a brain constituent that binds to the cannabinoid receptor. Science 258(5090), 1946-1949 (1992).

2. Deutsch, D.G., Glaser, S.T., Howell, J.M., et al. The cellular uptake of anandamide is coupled to its breakdown by fatty-acid amide hydrolase. The Journal of Biological Chemisty 276(10), 6967-6973 (2001).

3. López-Rodriguez, M.L., Viso, A., Ortega-Gutiérrez, S., et al. Design, synthesis, and biological evaluation of new endocannabinoid transporter inhibitors. Eur. J. Med. Chem. 38(4), 403-412 (2003).

4. de Lago, E., Fernandez-Ruiz, J., Ortega-Gutiérrez, S., et al. UCM707, a potent and selective inhibitor of endocannabinoid uptake, potentiates hypokinetic and antinociceptive effects of anandamide. Eur. J. Pharmacol. 449(1-2), 99-103 (2002).