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.

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.

Association of Cannabinoid Administration With Experimental Pain in Healthy Adults: A Systematic Review and Meta-analysis

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.

Cannabinoid Receptor Type 1 and Its Role as an Analgesic: An Opioid Alternative?

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.

Synthetic Cannabinoid Receptor Agonists and Antagonists: Implication in CNS Disorders.

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.

Targeting Peripherally Restricted Cannabinoid Receptor 1, Cannabinoid Receptor 2, and Endocannabinoid-Degrading Enzymes for the Treatment of Neuropathic Pain Including Neuropathic Orofacial Pain

This review will discuss the above-mentioned alternative approaches that show potential for treating neuropathic pain including NOP, including inhibition of degradation of a major endocannabinoid, 2-arachydonoylglycerol, which can attenuate NOP following trigeminal nerve injury in mice.

The cannabinoid agonist CB-13 produces peripherally mediated analgesia in mice but elicits tolerance and signs of CNS activity with repeated dosing

Significant caution is warranted regarding therapeutic use of CB-13 with the goal of avoiding CNS side effects, but the clear analgesic effect of acute peripheral CB1 receptor activation suggests that peripherally restricted cannabinoids are a viable target for novel analgesic development.



Lack of effect of central nervous system‐active doses of nabilone on capsaicin‐induced pain and hyperalgesia

The aim of the present study was to investigate the effects of nabilone on capsaicin‐induced pain and hyperalgesia, as well as on biomarkers of cannabinoid central nervous system (CNS) effects. A

Dose-dependent Effects of Smoked Cannabis on Capsaicin-induced Pain and Hyperalgesia in Healthy Volunteers

There is a window of modest analgesia for smoked cannabis, with lower doses decreasing pain and higher doses increasing pain, this study suggests.

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.

Analgesic effect of the synthetic cannabinoid CT-3 on chronic neuropathic pain: a randomized controlled trial.

In this preliminary study, CT-3 was effective in reducing chronic neuropathic pain compared with placebo and no major adverse effects were observed.

Effects of nabilone, a synthetic cannabinoid, on postoperative pain

  • P. Beaulieu
  • Medicine
    Canadian journal of anaesthesia = Journal canadien d'anesthesie
  • 2006
High dose nabilone in the presence of morphine patient controlled analgesia is associated with an increase in pain scores in patients undergoing major surgery, contrary to the main hypothesis.

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

This review focuses on the analgesic potential of CB2 receptor agonists for inflammatory, post-operative and neuropathic pain states and discusses their possible sites and mechanisms of action.