Fluorinated cannabidiol derivatives: Enhancement of activity in mice models predictive of anxiolytic, antidepressant and antipsychotic effects

Aviva Breuer, Christeene G. Haj, Manoela V. Fogaça, Felipe V. Gomes, Nicole Rodrigues Silva, João Francisco Pedrazzi, Elaine A.Del Bel, Jaime C. Hallak, José A. Crippa, Antonio W. Zuardi, Raphael Mechoulam, Francisco S. Guimarães

Research output: Contribution to journalArticlepeer-review

42 Scopus citations

Abstract

Cannabidiol (CBD) is a major Cannabis sativa constituent, which does not cause the typical marijuana psychoactivity. However, it has been shown to be active in a numerous pharmacological assays, including mice tests for anxiety, obsessive-compulsive disorder, depression and schizophrenia. In human trials the doses of CBD needed to achieve effects in anxiety and schizophrenia are high. We report now the synthesis of 3 fluorinated CBD derivatives, one of which, 4'-F-CBD (HUF-101) (1), is considerably more potent than CBD in behavioral assays in mice predictive of anxiolytic, antidepressant, antipsychotic and anticompulsive activity. Similar to CBD, the anti-compulsive effects of HUF-101 depend on cannabinoid receptors.

Original languageAmerican English
Article numbere0158779
JournalPLoS ONE
Volume11
Issue number7
DOIs
StatePublished - Jul 2016

Bibliographical note

Publisher Copyright:
© 2016 Breuer et al.This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

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