During the last years the development of approaches to multitarget drug design and discovery is gaining acceptance.
The cannabinoids are potentially excellent multi-target drug candidates because of their interesting pharmacological
profiles, among which stands out the dual capacity of cannabinoid ligands to act as cannabinoid agonist and cholinesterase
inhibitors. In this article, inhibition, kinetics studies and docking simulations with a representative set of cannabinoids are
presented. The results of these studies showed the inhibitory capacity of some agonist cannabinoids with selectivity at
AChE or BuChE enzymes. The kinetic and modelling studies allowed us to postulate the potential mode of action and the
binding site of the cannabinoids. In general, the studied cannabinoids showed a mixed type inhibition mode of action. The
exception to this behaviour was found for the agonist CP-55,940 that showed a non-competitive inhibition, suggesting that
this cannabinoid only binds to the peripheral site.