Special Issue "Cannabinoids as Medicines"

A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: closed (30 November 2018)

Special Issue Editor

Guest Editor
Prof. Dr. Gary J. Stephens

School of Pharmacy, University of Reading, Whiteknights, PO Box 228, Reading RG6 6AJ, UK
Website | E-Mail
Interests: electrophysiology; voltage-gated calcium channels; cannabinoids; ion channels; GPCRs; pain; ataxia

Special Issue Information

Dear Colleagues,

The last three decades have seen real advances in the characterization of the body’s endocannabinoid system, with detailed knowledge of cannabinoid receptor subtypes, endocannabinoid metabolic pathways and their cell signaling pathways. In parallel, advocacy, and some sanction, of the use of medicinal marijuana, often based on anecdotal evidence, has become a pertinent topic of societal and scientific debate. At a scientific level, interest has tended to shift away from use of Δ9-tetrahydrocannabinol (THC), due to its psychoactive intoxicant effects, towards alternative plant-derived phytocannabinoids or synthetic cannabinoids and their potential therapeutic applications. Despite some high-profile clinical failures, recent well-controlled clinical trials have begun to advance non-THC cannabinoids towards human therapeutic use. Authors are invited to submit original and review articles of basic science, preclinical and clinical findings contributing to the understanding of the current state of play and future potential for cannabinoids as medicines to be published in this Special Issue of Pharmaceuticals.

Prof. Dr. Gary J. Stephens
Guest Editor

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access quarterly journal published by MDPI.

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Keywords

  • endocannabinoids
  • phytocannabinoids
  • cannabinoid therapy

Published Papers (3 papers)

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Research

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Open AccessArticle Controlled-Deactivation CB1 Receptor Ligands as a Novel Strategy to Lower Intraocular Pressure
Pharmaceuticals 2018, 11(2), 50; https://doi.org/10.3390/ph11020050
Received: 28 April 2018 / Revised: 13 May 2018 / Accepted: 18 May 2018 / Published: 22 May 2018
Cited by 1 | PDF Full-text (2453 KB) | HTML Full-text | XML Full-text
Abstract
Nearly half a century has passed since the demonstration that cannabis and its chief psychoactive component Δ9-THC lowers intraocular pressure (IOP). Elevated IOP remains the chief hallmark and therapeutic target for glaucoma, a condition that places millions at risk of blindness. [...] Read more.
Nearly half a century has passed since the demonstration that cannabis and its chief psychoactive component Δ9-THC lowers intraocular pressure (IOP). Elevated IOP remains the chief hallmark and therapeutic target for glaucoma, a condition that places millions at risk of blindness. It is likely that Δ9-THC exerts much of its IOP-lowering effects via the activation of CB1 cannabinoid receptors. However, the initial promise of CB1 as a target for treating glaucoma has not thus far translated into a credible therapeutic strategy. We have recently shown that blocking monoacylglycerol lipase (MAGL), an enzyme that breaks the endocannabinoid 2-arachidonoyl glycerol (2-AG), substantially lowers IOP. Another strategy is to develop cannabinoid CB1 receptor agonists that are optimized for topical application to the eye. Recently we have reported on a controlled-deactivation approach where the “soft” drug concept of enzymatic deactivation was combined with a “depot effect” that is commonly observed with Δ9-THC and other lipophilic cannabinoids. This approach allowed us to develop novel cannabinoids with a predictable duration of action and is particularly attractive for the design of CB1 activators for ophthalmic use with limited or no psychoactive effects. We have tested a novel class of compounds using a combination of electrophysiology in autaptic hippocampal neurons, a well-characterized model of endogenous cannabinoid signaling, and measurements of IOP in a mouse model. We now report that AM7410 is a reasonably potent and efficacious agonist at CB1 in neurons and that it substantially (30%) lowers IOP for as long as 5 h after a single topical treatment. This effect is absent in CB1 knockout mice. Our results indicate that the direct targeting of CB1 receptors with controlled-deactivation ligands is a viable approach to lower IOP in a murine model and merits further study in other model systems. Full article
(This article belongs to the Special Issue Cannabinoids as Medicines)
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Review

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Open AccessReview Endocannabinoids in Body Weight Control
Pharmaceuticals 2018, 11(2), 55; https://doi.org/10.3390/ph11020055
Received: 28 April 2018 / Revised: 17 May 2018 / Accepted: 28 May 2018 / Published: 30 May 2018
Cited by 3 | PDF Full-text (2079 KB) | HTML Full-text | XML Full-text
Abstract
Maintenance of body weight is fundamental to maintain one’s health and to promote longevity. Nevertheless, it appears that the global obesity epidemic is still constantly increasing. Endocannabinoids (eCBs) are lipid messengers that are involved in overall body weight control by interfering with manifold [...] Read more.
Maintenance of body weight is fundamental to maintain one’s health and to promote longevity. Nevertheless, it appears that the global obesity epidemic is still constantly increasing. Endocannabinoids (eCBs) are lipid messengers that are involved in overall body weight control by interfering with manifold central and peripheral regulatory circuits that orchestrate energy homeostasis. Initially, blocking of eCB signaling by first generation cannabinoid type 1 receptor (CB1) inverse agonists such as rimonabant revealed body weight-reducing effects in laboratory animals and men. Unfortunately, rimonabant also induced severe psychiatric side effects. At this point, it became clear that future cannabinoid research has to decipher more precisely the underlying central and peripheral mechanisms behind eCB-driven control of feeding behavior and whole body energy metabolism. Here, we will summarize the most recent advances in understanding how central eCBs interfere with circuits in the brain that control food intake and energy expenditure. Next, we will focus on how peripheral eCBs affect food digestion, nutrient transformation and energy expenditure by interfering with signaling cascades in the gastrointestinal tract, liver, pancreas, fat depots and endocrine glands. To finally outline the safe future potential of cannabinoids as medicines, our overall goal is to address the molecular, cellular and pharmacological logic behind central and peripheral eCB-mediated body weight control, and to figure out how these precise mechanistic insights are currently transferred into the development of next generation cannabinoid medicines displaying clearly improved safety profiles, such as significantly reduced side effects. Full article
(This article belongs to the Special Issue Cannabinoids as Medicines)
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Open AccessReview A Systematic Review and Meta-Analysis of the In Vivo Haemodynamic Effects of Δ9-Tetrahydrocannabinol
Pharmaceuticals 2018, 11(1), 13; https://doi.org/10.3390/ph11010013
Received: 4 December 2017 / Revised: 25 January 2018 / Accepted: 26 January 2018 / Published: 31 January 2018
Cited by 2 | PDF Full-text (3562 KB) | HTML Full-text | XML Full-text
Abstract
9-Tetrahydrocannabinol (THC) has complex effects on the cardiovascular system. We aimed to systematically review studies of THC and haemodynamic alterations. PubMed, Medline, and EMBASE were searched for relevant studies. Changes in blood pressure (BP), heart rate (HR), and blood flow (BF) [...] Read more.
9-Tetrahydrocannabinol (THC) has complex effects on the cardiovascular system. We aimed to systematically review studies of THC and haemodynamic alterations. PubMed, Medline, and EMBASE were searched for relevant studies. Changes in blood pressure (BP), heart rate (HR), and blood flow (BF) were analysed using the Cochrane Review Manager Software. Thirty-one studies met the eligibility criteria. Fourteen publications assessed BP (number, n = 541), 22 HR (n = 567), and 3 BF (n = 45). Acute THC dosing reduced BP and HR in anaesthetised animals (BP, mean difference (MD) −19.7 mmHg, p < 0.00001; HR, MD −53.49 bpm, p < 0.00001), conscious animals (BP, MD −12.3 mmHg, p = 0.0007; HR, MD −30.05 bpm, p < 0.00001), and animal models of stress or hypertension (BP, MD −61.37 mmHg, p = 0.03) and increased cerebral BF in murine stroke models (MD 32.35%, p < 0.00001). Chronic dosing increased BF in large arteries in anaesthetised animals (MD 21.95 mL/min, p = 0.05) and reduced BP in models of stress or hypertension (MD −22.09 mmHg, p < 0.00001). In humans, acute administration increased HR (MD 8.16 bpm, p < 0.00001). THC acts differently according to species and experimental conditions, causing bradycardia, hypotension and increased BF in animals; and causing increased HR in humans. Data is limited, and further studies assessing THC-induced haemodynamic changes in humans should be considered. Full article
(This article belongs to the Special Issue Cannabinoids as Medicines)
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