Fluorinated Cannabidiol Derivatives: Enhancement of Activity in Mice Models Predictive of Anxiolytic, Antidepressant and Antipsychotic Effects

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 t...

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Bibliographic Details
Published in:PloS one 2016-07, Vol.11 (7), p.e0158779
Main Authors: Breuer, Aviva, Haj, Christeene G, Fogaça, Manoela V, Gomes, Felipe V, Silva, Nicole Rodrigues, Pedrazzi, João Francisco, Del Bel, Elaine A, Hallak, Jaime C, Crippa, José A, Zuardi, Antonio W, Mechoulam, Raphael, Guimarães, Francisco S
Format: Article
Language:English
Subjects:
Analysis
Animal models
Animals
Anti-Anxiety Agents - pharmacology
Antianxiety agents
Antidepressants
Antidepressive Agents - pharmacology
Antidepressive Agents - therapeutic use
Antipsychotic Agents - pharmacology
Antipsychotic Agents - therapeutic use
Antipsychotic drugs
Antipsychotics
Anxiety
Anxiety - drug therapy
Anxiety Disorders - drug therapy
Behavior, Animal - drug effects
Biology and Life Sciences
Cannabidiol - pharmacology
Cannabidiol - therapeutic use
Cannabinoid receptors
Cannabinoids
Cannabis
Cannabis sativa
Depression - drug therapy
Depressive Disorder - drug therapy
Derivatives
Disease Models, Animal
Drug dosages
Fluorination
Fluorine
Male
Marble
Marijuana
Medical schools
Medicine and Health Sciences
Mental depression
Mental disorders
Mice
Motor Activity - drug effects
Neurosciences
Obsessive compulsive disorder
Pharmacology
Physical Sciences
Psychopharmacology
Psychotropic drugs
Receptors
Research and Analysis Methods
Rodents
Schizophrenia
Schizophrenia - drug therapy
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Summary: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 anti-compulsive activity. Similar to CBD, the anti-compulsive effects of HUF-101 depend on cannabinoid receptors.
ISSN:1932-6203
1932-6203
DOI:10.1371/journal.pone.0158779