Effects of cannabidiol on the function of α7-nicotinic acetylcholine receptors

Mahgoub, Mohamed; Keun-Hang, Susan Yang; Sydorenko, Vadym; Ashoor, Abrar; Kabbani, Nadine; Kury, Lina Al; Sadek, Bassem; Howarth, Christopher F.; Isaev, Dmytro; Galadari, Sehamuddin; Öz, Murat

doi:10.1016/j.ejphar.2013.10.011

Cited by 71 publications

(45 citation statements)

References 49 publications

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“…Furthermore, CBD (1-30 μM) inhibited acetylcholine-induced ion currents recorded in rat hippocampal slices (IC 50 = 12.7 μM) [27].…”

Section: Nicotinic Acetylcholine Receptormentioning

confidence: 93%

“…Evidence that CBD modulates nicotinic acetylcholine receptor (nAchRs) function comes from a study by Mahgoub et al [27]. Electrophysiological recordings from Xenopus oocytes expressing the α-7-nAChR reveal a concentration-dependent inhibition in the presence of CBD (0.1-100.0 μM; Table 1).…”

Section: Nicotinic Acetylcholine Receptormentioning

confidence: 99%

“…Α4β2 and α7 nAchRs are potently inhibited by CBD [27]. As rapid desensitization of either subtype reduces dyskinesia [174], it is possible that the blockade of these receptors by CBD is responsible for its antidyskinetic effect.…”

Section: Cbd Receptor Targets In Movement Disordersmentioning

confidence: 99%

“…Although the activation of α-7-nACh receptor has been reported as anti-inflammatory and protective against nociception in neuropathic pain [262][263][264][265], it is unlikely that the analgesic proprieties of CBD are mediated by this receptor as CBD tends to antagonize (IC 50 = 12.7 μM) its action in vitro [27].…”

Section: Cbd Receptor Targets In Painmentioning

confidence: 99%

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Molecular Targets of Cannabidiol in Neurological Disorders

Bih

Chen

Nunn³

et al. 2015

Neurotherapeutics

462

323

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Cannabis has a long history of anecdotal medicinal use and limited licensed medicinal use. Until recently, alleged clinical effects from anecdotal reports and the use of licensed cannabinoid medicines are most likely mediated by tetrahydrocannabinol by virtue of: 1) this cannabinoid being present in the most significant quantities in these preparations; and b) the proportion:potency relationship between tetrahydrocannabinol and other plant cannabinoids derived from cannabis. However, there has recently been considerable interest in the therapeutic potential for the plant cannabinoid, cannabidiol (CBD), in neurological disorders but the current evidence suggests that CBD does not directly interact with the endocannabinoid system except in vitro at supraphysiological concentrations. Thus, as further evidence for CBD's beneficial effects in neurological disease emerges, there remains an urgent need to establish the molecular targets through which it exerts its therapeutic effects. Here, we conducted a systematic search of the extant literature for original articles describing the molecular pharmacology of CBD. We critically appraised the results for the validity of the molecular targets proposed. Thereafter, we considered whether the molecular targets of CBD identified hold therapeutic potential in relevant neurological diseases. The molecular targets identified include numerous classical ion channels, receptors, transporters, and enzymes. Some CBD effects at these targets in in vitro assays only manifest at high concentrations, which may be difficult to achieve in vivo, particularly given CBD's relatively poor bioavailability. Moreover, several targets were asserted through experimental designs that demonstrate only correlation with a given target rather than a causal proof. When the molecular targets of CBD that were physiologically plausible were considered for their potential for exploitation in neurological therapeutics, the results were variable. In some cases, the targets identified had little or no established link to the diseases considered. In others, molecular targets of CBD were entirely consistent with those already actively exploited in relevant, clinically used, neurological treatments. Finally, CBD was found to act upon a number of targets that are linked to neurological therapeutics but that its actions were not consistent withmodulation of such targets that would derive a therapeutically beneficial outcome. Overall, we find that while >65 discrete molecular targets have been reported in the literature for CBD, a relatively limited number represent plausible targets for the drug's action in neurological disorders when judged by the criteria we set. We conclude that CBD is very unlikely to exert effects in neurological diseases through modulation of the endocannabinoid system. Moreover, a number of other molecular targets of CBD reported in the literature are unlikely to be of relevance owing to effects only being observed at supraphysiological concentrations. Of interest and after excludin...

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“…Furthermore, CBD (1-30 μM) inhibited acetylcholine-induced ion currents recorded in rat hippocampal slices (IC 50 = 12.7 μM) [27].…”

Section: Nicotinic Acetylcholine Receptormentioning

confidence: 93%

Section: Nicotinic Acetylcholine Receptormentioning

confidence: 99%

Section: Cbd Receptor Targets In Movement Disordersmentioning

confidence: 99%

Section: Cbd Receptor Targets In Painmentioning

confidence: 99%

See 2 more Smart Citations

Molecular Targets of Cannabidiol in Neurological Disorders

Bih

Chen

Nunn³

et al. 2015

Neurotherapeutics

462

323

View full text Add to dashboard Cite

show abstract

“…There are several possible explanations for these effects of cannabidiol. Apart from its antagonism at CB 1 /CB 2 receptors, cannabidiol also acts as an inhibitor of fatty acid amide hydrolase (FAAH-enzyme that degrades anandamide) [77,110], but also as an antagonist at α7 nAChRs [111].…”

Section: Human Studiesmentioning

confidence: 99%

Cannabinoid-Nicotine Interactions

Auber

Justinová

Scherma

et al. 2015

Cannabinoid Modulation of Emotion, Memory, and Motivation

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Although nicotine and delta-9-tetrahydrocannabinol (THC), the main psychoactive ingredients in tobacco and cannabis, bind to different receptors in the brain, they have several features in common. Each of these drugs is typically selfadministered by smoking, and this behavior is maintained by rewarding effects that are mediated by brain circuitry that at least partially overlaps between the drugs. Each tends to be used chronically, leading to dependence and addiction in many users. Perhaps most importantly, the nicotinic and cannabinergic systems appear to interact in such a way that modulating one system can enhance or counteract effects of the other system. Therefore, studying cannabinoid-nicotine interactions could potentially lead to new treatments for addiction. This chapter considers such interactions, focusing on recent preclinical work that suggests manipulating the cannabinoid system can counteract the addictive effects of nicotine that manipulating the nicotinic system can counteract the addictive effects of cannabis, and that prior or concurrent use of cannabis has the detrimental effect of increasing the addictive effects of nicotine. Interactive effects of these systems on anxiety and memory are also considered, although these have been studied less than addiction-related effects.

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A critical review of cannabis in medicine and dentistry: A look back and the path forward

Abidi

Alghamdi

Derefinko

2022

Clinical & Exp Dental Res

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Introduction: In the last two decades, our understanding of the therapeutic utility and medicinal properties of cannabis has greatly changed. This change has been accompanied by widespread cannabis use in various communities and different age groups, especially within the United States. With this increase, we should consider the potential effects of cannabis-hemp on general public health and how they could alter therapeutic outcomes. Material and Methods:The present investigation examined cannabis use for recreational and therapeutic use and a review of pertinent indexed literature was performed. The focused question evaluates "how cannabis or hemp products impact health parameters and do they provide potential therapeutic value in dentistry, and how do they interact with conventional medicines (drugs)." Indexed databases (PubMed/Medline, EMBASE) were searched without any time restrictions but language was restricted to English. Results:The review highlights dental concerns of cannabis usage, the need to understand the endocannabinoid system (ECS), cannabinoid receptor system, its endogenous ligands, pharmacology, metabolism, current oral health, and medical dilemma to ascertain the detrimental or beneficial effects of using cannabis-hemp products. The pharmacological effects of pure cannabidiol (CBD) have been studied extensively while cannabis extracts can vary significantly and lack empirical studies.Several metabolic pathways are affected by cannabis use and could pose a potential drug interaction. The chronic use of cannabis is associated with health issues, but the therapeutic potential is multifold since there is a regulatory role of ECS in many pathologies.

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Effects of cannabidiol on the function of α7-nicotinic acetylcholine receptors

Cited by 71 publications

References 49 publications

Molecular Targets of Cannabidiol in Neurological Disorders

Molecular Targets of Cannabidiol in Neurological Disorders

Cannabinoid-Nicotine Interactions

A critical review of cannabis in medicine and dentistry: A look back and the path forward

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