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Evaluation of phytocannabinoids from high-potency Cannabis sativa using in vitro bioassays to determine structure–activity relationships for cannabinoid receptor 1 and cannabinoid receptor 2

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Cannabis has been around for thousands of years and has been used recreationally, medicinally, and for fiber. Over 500 compounds have been isolated from Cannabis sativa with approximately 105 being cannabinoids. Of those 105 compounds, Δ9-tetrahydrocannabinol has been determined as the primary constituent, which is also responsible for the psychoactivity associated with Cannabis. Cannabinoid receptors belong to the large superfamily of G protein-coupled receptors. Targeting the cannabinoid receptors has the potential to treat a variety of conditions such as pain, neurodegeneration, appetite, immune function, anxiety, cancer, and others. Developing in vitro bioassays to determine binding and functional activity of compounds has the ability to lead researchers to develop a safe and effective drug that may target the cannabinoid receptors. Using radioligand binding and functional bioassays, a structure–activity relationship for major and minor cannabinoids was developed.

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This study was supported by Grant Number P20GM104931 from the National Institute of General Medical Sciences (NIGMS), a component of the National Institutes of Health (NIH) and its contents are solely the responsibility of the authors and do not necessarily represent the official view of NIGMS or NIH. This investigation was conducted in a facility constructed with support from research facilities improvement program C06RR14503 from the NIH National Center for Research Resources.

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Correspondence to Stephen J. Cutler.

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Husni, A.S., McCurdy, C.R., Radwan, M.M. et al. Evaluation of phytocannabinoids from high-potency Cannabis sativa using in vitro bioassays to determine structure–activity relationships for cannabinoid receptor 1 and cannabinoid receptor 2. Med Chem Res 23, 4295–4300 (2014).

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