Multitarget Cannabinoids as Novel Strategy for Alzheimer Disease

Author(s): Pedro Gonzalez-Naranjo, Nuria E. Campillo, Concepcion Perez, Juan A. Paez

Journal Name: Current Alzheimer Research

Volume 10 , Issue 3 , 2013

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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.

Keywords: Alzheimer disease, agonist cannabinoids, cholinesterase inhibitors, multitarget drugs

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Article Details

Year: 2013
Published on: 01 April, 2013
Page: [229 - 239]
Pages: 11
DOI: 10.2174/1567205011310030002
Price: $65

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