MDA7: a novel selective agonist for CB2 receptors that prevents allodynia in rat neuropathic pain models
Open accessAbstract
BACKGROUND AND PURPOSE: There is growing interest in using cannabinoid type 2 (CB(2)) receptor agonists for the treatment of neuropathic pain. In this report, we describe the pharmacological characteristics of MDA7 (1-[(3-benzyl-3-methyl-2,3-dihydro-1-benzofuran-6-yl)carbonyl]piperidine), a novel CB(2) receptor agonist. EXPERIMENTAL APPROACH: We characterized the pharmacological profile of MDA7 by using radioligand-binding assays and in vitro functional assays at human cannabinoid type 1 (CB(1)) and CB(2) receptors. In vitro functional assays were performed at rat CB(1) and CB(2) receptors. The effects of MDA7 in reversing neuropathic pain were assessed in spinal nerve ligation and paclitaxel-induced neuropathy models in rats. KEY RESULTS: MDA7 exhibited selectivity and agonist affinity at human and rat CB(2) receptors. MDA7 treatment attenuated tactile allodynia produced by spinal nerve ligation or by paclitaxel in a dose-related manner. These effects were selectively antagonized by a CB(2) receptor antagonist but not by CB(1) or opioid receptor antagonists. MDA7 did not affect rat locomotor activity. CONCLUSION AND IMPLICATIONS: MDA7, a novel selective CB(2) agonist, was effective in suppressing neuropathic nociception in two rat models without affecting locomotor behaviour. These results confirm the potential for CB(2) agonists in the treatment of neuropathic pain.
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
The CB2 agonist AM1241 suppresses both thermal hyperalgesia and mechanical allodynia following SNL in both rats and mice.
“The CB2 agonist AM1241 suppresses both thermal hyperalgesia and mechanical allodynia following SNL in both rats17, 44, 85 and mice44.”
From Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside (2009) · cites this paper as [85]
A more recent study using the same paclitaxel dosing paradigm reported the presence of mechanical allodynia and the absence of thermal hyperalgesia.
“A more recent study using the same paclitaxel dosing paradigm118 reported the presence of mechanical allodynia and the absence of thermal hyperalgesia.85”
From Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside (2009) · cites this paper as [85]
MDA7 suppressed paclitaxel-induced mechanical allodynia, although mediation by CB2 receptors was not assessed.
“Naguib and colleagues85 demonstrated that a novel CB2-specific agonist, MDA7, suppressed paclitaxel-induced mechanical allodynia, although mediation by CB2 receptors was not assessed.”
From Cannabinoids as Pharmacotherapies for Neuropathic Pain: From the Bench to the Bedside (2009) · cites this paper as [85]
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
The citation lists haven’t been fetched yet
References 72 · Cited by 82
- Authors
- Naguib, M., Diaz, P., Xu, J. J., Astruc‐Diaz, F., Craig, S., Vivas‐Mejia, P., & Brown, D. L.
- Affiliations
- The University of Texas MD Anderson Cancer Center (US)
- Corresponding author
- Naguib, M
- Venue
- British Journal of Pharmacology
- Publisher
- Wiley
- Published
- 2008-12
- Volume
- 155
- Issue
- 7
- Pages
- 1104-1116
- ISSN
- 0007-1188 (ISSN-L)
- 1476-5381
- PMC
- PMC2597252
- OpenAlex
- W1512522134
- Cited by
- 82
- References
- 72
- Citations by year
- 2026: 4 · 2025: 5 · 2024: 3 · 2023: 6 · 2022: 4 · 2021: 6 · 2020: 1 · 2019: 2 · 2018: 3 · 2017: 2 · 2016: 4 · 2015: 3 · 2014: 3 · 2013: 9 · 2012: 10
- FWCI
- 4.22
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- British Journal of Pharmacology (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
- Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
- Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
- Keywords
- CB2 receptor agonist, neuropathic pain, allodynia, spinal nerve ligation, paclitaxel-induced peripheral neuropathy, CB1 receptor, locomotor activity, cannabinoid analgesia
- MeSH terms
- Analgesics, Animals, Benzofurans, Cricetulus, Disease Models, Animal, Dose-Response Relationship, Drug, Cricetinae, Humans, Ligation, Motor Activity, Neuralgia, Pain Measurement, Piperidines, Radioligand Assay, Species Specificity, Spinal Nerves, CHO Cells, Paclitaxel, Receptor, Cannabinoid, CB1, Receptor, Cannabinoid, CB2, Rats
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review
