Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy

Valenzano, Kenneth J.; Tafesse, Laykea; Lee, Gary; Harrison, James E.; Boulet, Jamie M.; Gottshall, Susan L.; Mark, Lilly; Pearson, Michelle S.; Miller, Wendy; Shan, Shen; Rabadi, Leyana; Rotshteyn, Yakov; Chaffer, Suzanne M.; Turchin, Paul I.; Elsemore, David A.; Toth, Mathew; Koetzner, Lee; Whiteside, Garth T.

doi:10.1016/j.neuropharm.2004.12.008

Cited by 288Cannabis and Cannabinoid ResearchPain Mechanisms and TreatmentsAdenosine and Purinergic Signaling

Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy

Valenzano, Kenneth J., Tafesse, Laykea, Lee, Gary, Harrison, James E., Boulet, Jamie M., Gottshall, Susan L., Mark, Lilly, Pearson, Michelle S. +10 more·2005·Neuropharmacology

DOI 10.1016/j.neuropharm.2004.12.008

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Abstract

To date, two cannabinoid receptors have been identified, CB1 and CB2. Activation of these receptors with non-selective cannabinoid receptor agonists reduces pain sensitivity in animals and humans. However, activation of CB1 receptors is also associated with central side effects, including ataxia and catalepsy. More recently, a role for selective CB2 agonists in pain modification has been demonstrated. GW405833, a selective CB2 agonist, was recently reported to partially reverse the inflammation and hyperalgesia in a rat model of acute inflammation. In the current report, we extend the characterization and therapeutic potential of this compound. For the first time, we show that GW405833 selectively binds both rat and human CB2 receptors with high affinity, where it acts as a partial agonist (approximately 50% reduction of forskolin-mediated cAMP production compared to the full cannabinoid agonist, CP55,940). We also report for the first time that intraperitoneal administration of GW405833 (0.3-100 mg/kg) to rats shows linear, dose-dependent increases in plasma levels and substantial penetration into the central nervous system. In addition, GW405833 (up to 30 mg/kg) elicits potent and efficacious antihyperalgesic effects in rodent models of neuropathic, incisional and chronic inflammatory pain, the first description of this compound in these models. In contrast, analgesia, sedation and catalepsy were not observed in this dose range, but were apparent at 100 mg/kg. Additionally, GW405833 was not antihyperalgesic against chronic inflammatory pain in CB2 knockout mice. These data support the tenet that selective CB2 receptor agonists have the potential to treat pain without eliciting the centrally-mediated side effects associated with non-selective cannabinoid agonists, and highlight the utility of GW405833 for the investigation of CB2 physiology.

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Acute administration of CB2 receptor agonists reduces CFA-induced mechanical and thermal hyperalgesia.
“Acute administration of CB 2 receptor agonists reduces CFA-induced mechanical and thermal hyperalgesia (Hsieh et al, 2011;Valenzano et al, 2005;Yao et al, 2008Yao et al, , 2009)).”
From The endogenous cannabinoid system: a budding source of targets for treating inflammatory and neuropathic pain (2018) · cites this paper as Valenzano et al, 2005

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Authors: Valenzano, K. J., Tafesse, L., Lee, G., Harrison, J. E., Boulet, J. M., Gottshall, S. L., Mark, L., Pearson, M. S., Miller, W., Shan, S., Rabadi, L., Rotshteyn, Y., Chaffer, S. M., Turchin, P. I., Elsemore, D. A., Toth, M., Koetzner, L., & Whiteside, G. T.
Affiliations: Purdue Pharma (United States) (US)
Corresponding author: Valenzano, Kenneth J.
ORCID: Tafesse, Laykea
Koetzner, Lee
Whiteside, Garth T.
Venue: Neuropharmacology
Publisher: Elsevier BV
Published: 2005-04
Volume: 48
Issue: 5
Pages: 658-672
ISSN: 0028-3908 (ISSN-L)
DOI: 10.1016/j.neuropharm.2004.12.008
OpenAlex: W2018656586
Cited by: 288
References: 41
Citations by year: 2026: 7 · 2025: 6 · 2024: 9 · 2023: 11 · 2022: 9 · 2021: 13 · 2020: 9 · 2019: 9 · 2018: 6 · 2017: 13 · 2016: 12 · 2015: 13 · 2014: 13 · 2013: 12 · 2012: 20
FWCI: 13.82
Type: journal article
Language: en
Open access: closed
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Neuropharmacology (publishedVersion)
PubMed (publishedVersion)
Topics: Health Sciences › Medicine › Pharmacology › Cannabis and Cannabinoid Research
Health Sciences › Medicine › Physiology › Pain Mechanisms and Treatments
Life Sciences › Biochemistry, Genetics and Molecular Biology › Physiology › Adenosine and Purinergic Signaling
Keywords: CB2 receptor, CB2 receptor agonist, partial agonists, pharmacokinetics, CNS penetration, antihyperalgesia, neuropathic pain, incisional pain, chronic inflammatory pain, CB2 knockout mice, catalepsy, ataxia, anxiety, sedation
MeSH terms: Gabapentin, Cyclic AMP, Amines, Analgesics, Animals, Anti-Inflammatory Agents, Non-Steroidal, Anxiety, Ataxia, Behavior, Animal, Binding, Competitive, Catalepsy, Cricetulus, Cyclohexanecarboxylic Acids, Cyclohexanols, Disease Models, Animal, Dose-Response Relationship, Drug, gamma-Aminobutyric Acid, Cricetinae, Humans, Immunosuppressive Agents, Indoles, Indomethacin, Inflammation, Male, Morpholines, Naphthalenes, Pain, Pain Measurement, Psychomotor Performance, Reaction Time, Time Factors, CHO Cells, Rats, Sprague-Dawley, Mice, Knockout, Excitatory Amino Acid Antagonists, Receptor, Cannabinoid, CB2, Benzoxazines, Mice, Rats

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Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy

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