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

نویسندگان

  • 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
چکیده

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.

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عنوان ژورنال:

دوره 11  شماره 

صفحات  -

تاریخ انتشار 2016