Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597).

  title={Pharmacological profile of the selective FAAH inhibitor KDS-4103 (URB597).},
  author={Daniele Piomelli and Giorgio Tarzia and Andrea Duranti and Andrea Tontini and Marco Mor and Timothy R Compton and Olivier Dasse and Edward P Monaghan and Jeff A. Parrott and David Putman},
  journal={CNS drug reviews},
  volume={12 1},
In the present article, we review the pharmacological properties of KDS-4103 (URB597), a highly potent and selective inhibitor of the enzyme fatty-acid amide hydrolase (FAAH), which catalyzes the intracellular hydrolysis of the endocannabinoid anandamide. In vitro, KDS-4103 inhibits FAAH activity with median inhibitory concentrations (IC(50)) of 5 nM in rat brain membranes and 3 nM in human liver microsomes. In vivo, KDS-4103 inhibits rat brain FAAH activity after intraperitoneal (i.p… CONTINUE READING
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