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Fluorinated Cannabidiol Derivatives: Enhancement of Activity in Mice Models Predictive of Anxiolytic, Antidepressant and Antipsychotic Effects.
PLoS One. 2016; 11(7):e0158779.Plos

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 anti-compulsive activity. Similar to CBD, the anti-compulsive effects of HUF-101 depend on cannabinoid receptors.

Authors+Show Affiliations

Institute for Drug Research, Medical Faculty, Hebrew University, Jerusalem, Israel.Institute for Drug Research, Medical Faculty, Hebrew University, Jerusalem, Israel.Departments of Pharmacology, Medical School of Ribeirão Preto, University of São Paulo, São Paulo, Brazil.Departments of Pharmacology, Medical School of Ribeirão Preto, University of São Paulo, São Paulo, Brazil.Departments of Pharmacology, Medical School of Ribeirão Preto, University of São Paulo, São Paulo, Brazil.Neuroscience and Behavior, Medical School of Ribeirão Preto, University of São Paulo, São Paulo, Brazil.Department of Morphology, Physiology and Pathology, School of Odontology of Ribeirão Preto, University of São Paulo, São Paulo, Brazil.Neuroscience and Behavior, Medical School of Ribeirão Preto, University of São Paulo, São Paulo, Brazil.Neuroscience and Behavior, Medical School of Ribeirão Preto, University of São Paulo, São Paulo, Brazil.Neuroscience and Behavior, Medical School of Ribeirão Preto, University of São Paulo, São Paulo, Brazil.Institute for Drug Research, Medical Faculty, Hebrew University, Jerusalem, Israel.Departments of Pharmacology, Medical School of Ribeirão Preto, University of São Paulo, São Paulo, Brazil.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

27416026

Citation

Breuer, Aviva, et al. "Fluorinated Cannabidiol Derivatives: Enhancement of Activity in Mice Models Predictive of Anxiolytic, Antidepressant and Antipsychotic Effects." PloS One, vol. 11, no. 7, 2016, pp. e0158779.
Breuer A, Haj CG, Fogaça MV, et al. Fluorinated Cannabidiol Derivatives: Enhancement of Activity in Mice Models Predictive of Anxiolytic, Antidepressant and Antipsychotic Effects. PLoS One. 2016;11(7):e0158779.
Breuer, A., Haj, C. G., Fogaça, M. V., Gomes, F. V., Silva, N. R., Pedrazzi, J. F., Del Bel, E. A., Hallak, J. C., Crippa, J. A., Zuardi, A. W., Mechoulam, R., & Guimarães, F. S. (2016). Fluorinated Cannabidiol Derivatives: Enhancement of Activity in Mice Models Predictive of Anxiolytic, Antidepressant and Antipsychotic Effects. PloS One, 11(7), e0158779. https://doi.org/10.1371/journal.pone.0158779
Breuer A, et al. Fluorinated Cannabidiol Derivatives: Enhancement of Activity in Mice Models Predictive of Anxiolytic, Antidepressant and Antipsychotic Effects. PLoS One. 2016;11(7):e0158779. PubMed PMID: 27416026.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fluorinated Cannabidiol Derivatives: Enhancement of Activity in Mice Models Predictive of Anxiolytic, Antidepressant and Antipsychotic Effects. AU - Breuer,Aviva, AU - Haj,Christeene G, AU - Fogaça,Manoela V, AU - Gomes,Felipe V, AU - Silva,Nicole Rodrigues, AU - Pedrazzi,João Francisco, AU - Del Bel,Elaine A, AU - Hallak,Jaime C, AU - Crippa,José A, AU - Zuardi,Antonio W, AU - Mechoulam,Raphael, AU - Guimarães,Francisco S, Y1 - 2016/07/14/ PY - 2016/05/09/received PY - 2016/06/21/accepted PY - 2016/7/15/entrez PY - 2016/7/16/pubmed PY - 2017/7/29/medline SP - e0158779 EP - e0158779 JF - PloS one JO - PLoS One VL - 11 IS - 7 N2 - 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. SN - 1932-6203 UR - https://www.unboundmedicine.com/medline/citation/27416026/Fluorinated_Cannabidiol_Derivatives:_Enhancement_of_Activity_in_Mice_Models_Predictive_of_Anxiolytic_Antidepressant_and_Antipsychotic_Effects_ L2 - https://dx.plos.org/10.1371/journal.pone.0158779 DB - PRIME DP - Unbound Medicine ER -