1. Fluorinated cannabidiol derivatives: enhancement of activity in mice models predictive of anxiolytic, antidepressant and antipsychotic effects
- Author
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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, and Francisco S Guimarães
- Subjects
Male ,Cannabinoid receptor ,Physiology ,medicine.medical_treatment ,lcsh:Medicine ,Anxiety ,Pharmacology ,Mice ,0302 clinical medicine ,Anti-Anxiety Agents ,Medicine and Health Sciences ,Cannabidiol ,Antipsychotics ,Biomechanics ,lcsh:Science ,Mammals ,Multidisciplinary ,Behavior, Animal ,Depression ,Drugs ,Antidepressants ,Animal Models ,Anxiety Disorders ,Antidepressive Agents ,Chemistry ,surgical procedures, operative ,Schizophrenia ,Behavioral Pharmacology ,Vertebrates ,Physical Sciences ,Antidepressant ,medicine.symptom ,Antipsychotic Agents ,medicine.drug ,Research Article ,Chemical Elements ,medicine.drug_class ,Motor Activity ,Research and Analysis Methods ,FARMACOLOGIA ,Anxiolytic ,digestive system ,Rodents ,03 medical and health sciences ,Model Organisms ,Recreational Drug Use ,medicine ,Animals ,Antipsychotic ,Swimming ,Depressive Disorder ,business.industry ,Biological Locomotion ,lcsh:R ,Amphetamines ,Organisms ,Correction ,Biology and Life Sciences ,Fluorine ,medicine.disease ,digestive system diseases ,030227 psychiatry ,Disease Models, Animal ,Amniotes ,lcsh:Q ,business ,030217 neurology & neurosurgery ,Anxiolytics - 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.
- Published
- 2016