TY - JOUR
T1 - Fluorinated cannabidiol derivatives
T2 - 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 - Bel, Elaine A.Del
AU - Hallak, Jaime C.
AU - Crippa, José A.
AU - Zuardi, Antonio W.
AU - Mechoulam, Raphael
AU - Guimarães, Francisco S.
N1 - 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.
PY - 2016/7
Y1 - 2016/7
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 anticompulsive activity. Similar to CBD, the anti-compulsive effects of HUF-101 depend on cannabinoid receptors.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=84978636526&partnerID=8YFLogxK
U2 - 10.1371/journal.pone.0158779
DO - 10.1371/journal.pone.0158779
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C2 - 27416026
AN - SCOPUS:84978636526
SN - 1932-6203
VL - 11
JO - PLoS ONE
JF - PLoS ONE
IS - 7
M1 - e0158779
ER -