Evaluation of the analgesic efficacy and psychoactive effects of AZD1940, a novel peripherally acting cannabinoid agonist, in human capsaicin‐induced pain and hyperalgesia

  title={Evaluation of the analgesic efficacy and psychoactive effects of AZD1940, a novel peripherally acting cannabinoid agonist, in human capsaicin‐induced pain and hyperalgesia},
  author={Jarkko Kalliom{\"a}ki and Peter Annas and Karin Huizar and Cyril P. Clarke and Annika Zettergren and Rolf Karlsten and M{\"a}rta Segerdahl},
  journal={Clinical and Experimental Pharmacology and Physiology},
The aim of the present study was to investigate the effects of AZD1940, a novel peripherally acting cannabinoid CB1/CB2 receptor agonist, on capsaicin‐induced pain and hyperalgesia, as well as on biomarkers of cannabinoid central nervous system (CNS) effects. The present study was a randomized, double‐blind, placebo‐controlled, four‐sequence, two‐period, cross‐over study in 44 male healthy volunteers aged 20–45 years. The effects of two single oral doses of AZD1940 (400 and 800 μg) were… 

Cannabinoid effects on responses to quantitative sensory testing among individuals with and without clinical pain: a systematic review.

This systematic review critically synthesizes the evidence for cannabinoid analgesic effects on quantitative sensory testing outcomes in both healthy adults and patients with chronic non-cancer pain (CNCP) and offers recommendations for future studies to improve study rigor and reproducibility.

Investigating the antinociceptive effects of N-docosahexaenoyl ethanolamine and novel kappa opioid receptor agonists

This thesis evaluated two classes of non-addictive compounds: bioactive lipids and kappa opioid receptor (KOPr) agonists and Salvinorin A (SalA), a selective KOPr agonist that has antinociceptive and anti-inflammatory effects in vivo, with limited abuse potential.

A data science approach to the selection of most informative readouts of the human intradermal capsaicin pain model to assess pregabalin effects

This study aimed at ranking the various readouts of a human capsaicin–based pain model with respect to the most relevant information about the effects of a potential reference analgesic and identified the pain intensities in the area of secondary hyperalgesia and of allodynia as the most suitable parameters to quantify the analgesic effects of pregabalin.

Descending serotonergic and noradrenergic systems do not regulate the antipruritic effects of cannabinoids*

Findings indicate that cannabinoids dose-dependently reduce serotonin-induced scratching behaviour and neurotoxic destruction of descending inhibitory pathways does not mediate this antipruritic effect of WIN 55,212-2.

Effect of styrene maleic acid WIN55,212-2 micelles on neuropathic pain in a rat model

The SMA-WIN micelle formulation was able to produce prolonged analgesia over a time when there was decreased impairment in the rotarod test compared with base WIN, and could potentially reduce the central nervous system effects of encapsulated WIN by limiting its transport across the blood–brain barrier.

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Cannabinoid drugs may prevent the onset of pain by producing small increases in pain thresholds but may not reduce the intensity of experimental pain already being experienced; instead, cannabinoids may make experimental pain feel less unpleasant and more tolerable, suggesting an influence on affective processes.

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Evidence is provided that one of the main roles of the endocannabinoid system is the regulation of gamma-aminobutyric acid (GABA) and/or glutamate release and its implications for pain.

The endocannabinoid system – current implications for drug development

  • C. Fowler
  • Biology, Medicine
    Journal of internal medicine
  • 2020
In this review, the state of the art for compounds affecting the endocannabinoid (eCB) system is described with a focus on the treatment of pain and dual‐acting compounds targeting this enzyme and other targets such as cyclooxygenase‐2 or transient potential vanilloid receptor 1 may be a way forward for the Treatment of pain.

Cannabinoids in pain management: CB1, CB2 and non-classic receptor ligands

  • Mellar P. Davis
  • Biology, Medicine
    Expert opinion on investigational drugs
  • 2014
Most clinically productive development of cannabinoids over the next 5 years will be in the area of selective CB2r agonists, which will be tested in various inflammatory, osteoarthritis and neuropathic pains.

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An overview of CB1 and CB2 receptor synthetic ligands obtained from drug research and in particular those synthesized for therapeutic purposes and potential clinical applications for central nervous system disorders is provided.



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Lack of Analgesia by Oral Standardized Cannabis Extract on Acute Inflammatory Pain and Hyperalgesia in Volunteers

The results suggest that cannabinoids are not effective analgesics for the treatment of acute nociceptive pain in humans and point to the development of a hyperalgesic state under cannabinoids.

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Cannabinoid CB2 Receptor-Mediated Anti-nociception in Models of Acute and Chronic Pain

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Dronabinol has a modest but clinically relevantanalgesic effect on central pain in patients with multiple sclerosis and on the SF-36 quality of life scale, the two items bodily pain and mental health indicated benefits from active treatment compared with placebo.