Tags

Type your tag names separated by a space and hit enter

Inhibition of inflammatory hyperalgesia by activation of peripheral CB2 cannabinoid receptors.
Anesthesiology. 2003 Oct; 99(4):955-60.A

Abstract

BACKGROUND

Cannabinoid receptor agonists inhibit inflammatory hyperalgesia in animal models. Nonselective cannabinoid receptor agonists also produce central nervous system (CNS) side effects. Agonists selective for CB2 cannabinoid receptors, which are not found in the CNS, do not produce the CNS effects typical of nonselective cannabinoid receptor agonists but do inhibit acute nociception. The authors used the CB2 receptor-selective agonist AM1241 to test the hypothesis that selective activation of peripheral CB2 receptors inhibits inflammatory hyperalgesia.

METHODS

Rats were injected in the hind paw with carrageenan or capsaicin. Paw withdrawal latencies were measured using a focused thermal stimulus. The effects of peripheral CB2 receptor activation were determined by using local injection of AM1241. CB2 receptor mediation of the actions of AM1241 was shown by using the CB2 receptor-selective antagonist AM630 and the CB1 receptor-selective antagonist AM251.

RESULTS

AM1241 fully reversed carrageenan-induced inflammatory thermal hyperalgesia when injected into the inflamed paw. In contrast, AM1241 injected into the contralateral paw had no effect, showing that its effects were local. AM1241 also reversed the local edema produced by hind paw carrageenan injection. The effects of AM1241 were reversed by the CB2 receptor-selective antagonist AM630, but not by the CB1 receptor-selective antagonist AM251. AM1241 also inhibited flinching and thermal hyperalgesia produced by hind paw capsaicin injection.

CONCLUSIONS

Local, peripheral CB2 receptor activation inhibits inflammation and inflammatory hyperalgesia. These results suggest that peripheral CB2 receptors may be an appropriate target for eliciting relief of inflammatory pain without the CNS effects of nonselective cannabinoid receptor agonists.

Authors+Show Affiliations

Department of Anesthesiology, The University of Arizona, Tucson, USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, U.S. Gov't, P.H.S.

Language

eng

PubMed ID

14508331

Citation

Quartilho, Aline, et al. "Inhibition of Inflammatory Hyperalgesia By Activation of Peripheral CB2 Cannabinoid Receptors." Anesthesiology, vol. 99, no. 4, 2003, pp. 955-60.
Quartilho A, Mata HP, Ibrahim MM, et al. Inhibition of inflammatory hyperalgesia by activation of peripheral CB2 cannabinoid receptors. Anesthesiology. 2003;99(4):955-60.
Quartilho, A., Mata, H. P., Ibrahim, M. M., Vanderah, T. W., Porreca, F., Makriyannis, A., & Malan, T. P. (2003). Inhibition of inflammatory hyperalgesia by activation of peripheral CB2 cannabinoid receptors. Anesthesiology, 99(4), 955-60.
Quartilho A, et al. Inhibition of Inflammatory Hyperalgesia By Activation of Peripheral CB2 Cannabinoid Receptors. Anesthesiology. 2003;99(4):955-60. PubMed PMID: 14508331.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Inhibition of inflammatory hyperalgesia by activation of peripheral CB2 cannabinoid receptors. AU - Quartilho,Aline, AU - Mata,Heriberto P, AU - Ibrahim,Mohab M, AU - Vanderah,Todd W, AU - Porreca,Frank, AU - Makriyannis,Alexandros, AU - Malan,T Philip,Jr PY - 2003/9/26/pubmed PY - 2003/10/30/medline PY - 2003/9/26/entrez SP - 955 EP - 60 JF - Anesthesiology JO - Anesthesiology VL - 99 IS - 4 N2 - BACKGROUND: Cannabinoid receptor agonists inhibit inflammatory hyperalgesia in animal models. Nonselective cannabinoid receptor agonists also produce central nervous system (CNS) side effects. Agonists selective for CB2 cannabinoid receptors, which are not found in the CNS, do not produce the CNS effects typical of nonselective cannabinoid receptor agonists but do inhibit acute nociception. The authors used the CB2 receptor-selective agonist AM1241 to test the hypothesis that selective activation of peripheral CB2 receptors inhibits inflammatory hyperalgesia. METHODS: Rats were injected in the hind paw with carrageenan or capsaicin. Paw withdrawal latencies were measured using a focused thermal stimulus. The effects of peripheral CB2 receptor activation were determined by using local injection of AM1241. CB2 receptor mediation of the actions of AM1241 was shown by using the CB2 receptor-selective antagonist AM630 and the CB1 receptor-selective antagonist AM251. RESULTS: AM1241 fully reversed carrageenan-induced inflammatory thermal hyperalgesia when injected into the inflamed paw. In contrast, AM1241 injected into the contralateral paw had no effect, showing that its effects were local. AM1241 also reversed the local edema produced by hind paw carrageenan injection. The effects of AM1241 were reversed by the CB2 receptor-selective antagonist AM630, but not by the CB1 receptor-selective antagonist AM251. AM1241 also inhibited flinching and thermal hyperalgesia produced by hind paw capsaicin injection. CONCLUSIONS: Local, peripheral CB2 receptor activation inhibits inflammation and inflammatory hyperalgesia. These results suggest that peripheral CB2 receptors may be an appropriate target for eliciting relief of inflammatory pain without the CNS effects of nonselective cannabinoid receptor agonists. SN - 0003-3022 UR - https://www.unboundmedicine.com/medline/citation/14508331/Inhibition_of_inflammatory_hyperalgesia_by_activation_of_peripheral_CB2_cannabinoid_receptors_ L2 - https://pubs.asahq.org/anesthesiology/article-lookup/doi/10.1097/00000542-200310000-00031 DB - PRIME DP - Unbound Medicine ER -