Antinociceptive effects of HUF-101, a fluorinated cannabidiol derivative

Silva, Nicole Rodrigues da; Gomes, Felipe V.; Fonseca, Miriam D.; Mechoulam, Raphael; Breuer, Aviva; Cunha, Thiago Mattar; Guimarães, Francisco Silveira

doi:10.1016/j.pnpbp.2017.07.012

Cited by 40 publications

(43 citation statements)

References 52 publications

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“…alone or in combination with morphine (Neelakantan et al, 2015). CBD reduced carrageenan-induced hyperalgesia (in a CB1 and CB2 dependent manner) and acetic acid-induced writhing (in a CB1 independent manner), but not hot-plate 13 analgesia, in mice (Silva et al, 2017). There is a clear need for broader study of the effects of CBD, including across routes of administration.…”

Section: Discussionmentioning

confidence: 99%

Vapor inhalation of cannabidiol (CBD) in rats

Javadi‐Paydar

Creehan²,

Kerr

et al. 2019

Preprint

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Cannabidiol (CBD), a compound found in many strains of the Cannabis genus, is increasingly available in e-cigarette liquids as well as other products. CBD use has been promoted for numerous purported benefits which have not been rigorously assessed in preclinical studies. To further validate an inhalation model to assess CBD effects in the rat. The primary goal was to determine plasma CBD levels after vapor inhalation and compare that with the levels observed after injection. Secondary goals were to determine if hypothermia is produced in male Sprague-Dawley rats and if CBD affects nociception measured by the warm water tail-withdrawal assay. Blood samples were collected from rats exposed for 30 minutes to vapor generated by an e-cigarette device using CBD (100, 400 mg/mL in the propylene glycol vehicle). Separate experiments assessed the body temperature response to CBD in combination with nicotine (30 mg/mL) and the anti-nociceptive response to CBD. Vapor inhalation of CBD produced concentration-related plasma CBD levels in male and female Wistar rats that were within the range of levels produced by 10 or 30 mg/kg, CBD, i.p.. Dose-related hypothermia was produced by CBD in male Sprague-Dawley rats, and nicotine (30 mg/mL) inhalation enhanced this effect. CBD inhalation had no effect on anti-nociception alone or in combination with Δ 9tetrahydrocannabinol inhalation. The vapor-inhalation approach is a suitable pre-clinical model for the investigation of the effects of inhaled CBD. This route of administration produces hypothermia in rats, while i.p. injection does not, at comparable plasma CBD levels.

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Section: Discussionmentioning

confidence: 99%

Vapor inhalation of cannabidiol (CBD) in rats

Javadi‐Paydar

Creehan²,

Kerr

et al. 2019

Preprint

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“…Moreover, Professor Raphael Mechoulam, from the Hebrew University of Jerusalem, responsible for the isolation and synthesis of major cannabinoids (including Δ9-THC in 1964 and CBD in 1963) and for the discovery of the endocannabinoid system (CB1 receptor in 1989 and anandamide in 1992), recently contacted the group to develop synthetic fluorinated analogs of CBD ( 158 , 159 ). These compounds have a strong potential for knowledge transfer to the productive sector, which could enable the commercialization of CBD-based products and offer the possibility of benefits for patients suffering from many of health conditions.…”

Section: New Age: From Clinical Trials With Cbd and Its Analogs To Momentioning

confidence: 99%

Translational Investigation of the Therapeutic Potential of Cannabidiol (CBD): Toward a New Age

et al. 2018

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Background: Among the many cannabinoids in the cannabis plant, cannabidiol (CBD) is a compound that does not produce the typical subjective effects of marijuana.Objectives: The aim of the present review is to describe the main advances in the development of the experimental and clinical use of cannabidiol CBD in neuropsychiatry.Methods: A non-systematic search was performed for studies dealing with therapeutic applications of CBD, especially performed by Brazilian researchers.Results: CBD was shown to have anxiolytic, antipsychotic and neuroprotective properties. In addition, basic and clinical investigations on the effects of CBD have been carried out in the context of many other health conditions, including its potential use in epilepsy, substance abuse and dependence, schizophrenia, social phobia, post-traumatic stress, depression, bipolar disorder, sleep disorders, and Parkinson.Discussion: CBD is an useful and promising molecule that may help patients with a number of clinical conditions. Controlled clinical trials with different neuropsychiatric populations that are currently under investigation should bring important answers in the near future and support the translation of research findings to clinical settings.

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“…The cannabinergic group of compounds includes CB1 or CB2 receptor ligands or blockers, substrates or inhibitors of fatty-acid amide hydrolase, and the endocannabinoid transporters. Studies of structure–activity relationships between endocannabinoid receptors and many synthesized cannabinergic compounds (e.g., phytocannabinoid analogues and derivatives) have been performed, along with the determination of cannabinergic biological activities and pharmacokinetic properties [ 6 , 7 , 8 ]. Cannabinergic compounds are considered as targets for the development of novel medications, e.g., for pain management [ 7 , 9 ] or as anti-inflammatory therapeutics [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

Chronological Review and Rational and Future Prospects of Cannabis-Based Drug Development

et al. 2020

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Despite the surge in cannabis chemistry research and its biological and medical activity, only a few cannabis-based pharmaceutical-grade drugs have been developed and marketed to date. Not many of these drugs are Food and Drug Administration (FDA)-approved, and some are still going through regulation processes. Active compounds including cannabinergic compounds (i.e., molecules targeted to modulate the endocannabinoid system) or phytocannabinoid analogues (cannabinoids produced by the plant) may be developed into single-molecule drugs. However, since in many cases treatment with whole-plant extract (whether as a solvent extraction, galenic preparation, or crude oil) is preferred over treatment with a single purified molecule, some more recently developed cannabis-derived drugs contain several molecules. Different combinations of active plant ingredients (API) from cannabis with proven synergies may be identified and developed as drugs to treat different medical conditions. However, possible negative effects between cannabis compounds should also be considered, as well as the effect of the cannabis treatment on the endocannabinoid system. FDA registration of single, few, or multiple molecules as drugs is a challenging process, and certain considerations that should be reviewed in this process, including issues of drug–drug interactions, are also discussed here.

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Antinociceptive effects of HUF-101, a fluorinated cannabidiol derivative

Cited by 40 publications

References 52 publications

Vapor inhalation of cannabidiol (CBD) in rats

Vapor inhalation of cannabidiol (CBD) in rats

Translational Investigation of the Therapeutic Potential of Cannabidiol (CBD): Toward a New Age

Chronological Review and Rational and Future Prospects of Cannabis-Based Drug Development

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