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The plant cannabinoid Delta9-tetrahydrocannabivarin can decrease signs of inflammation and inflammatory pain in mice.
Br J Pharmacol 2010; 160(3):677-87BJ

Abstract

BACKGROUND AND PURPOSE

The phytocannabinoid, Delta(9)-tetrahydrocannabivarin (THCV), can block cannabinoid CB(1) receptors. This investigation explored its ability to activate CB(2) receptors, there being evidence that combined CB(2) activation/CB(1) blockade would ameliorate certain disorders.

EXPERIMENTAL APPROACH

We tested the ability of THCV to activate CB(2) receptors by determining whether: (i) it inhibited forskolin-stimulated cyclic AMP production by Chinese hamster ovary (CHO) cells transfected with human CB(2) (hCB(2)) receptors; (ii) it stimulated [(35)S]GTPgammaS binding to hCB(2) CHO cell and mouse spleen membranes; (iii) it attenuated signs of inflammation/hyperalgesia induced in mouse hind paws by intraplantar injection of carrageenan or formalin; and (iv) any such anti-inflammatory or anti-hyperalgesic effects were blocked by a CB(1) or CB(2) receptor antagonist.

KEY RESULTS

THCV inhibited cyclic AMP production by hCB(2) CHO cells (EC(50)= 38 nM), but not by hCB(1) or untransfected CHO cells or by hCB(2) CHO cells pre-incubated with pertussis toxin (100 ng.mL(-1)) and stimulated [(35)S]GTPgammaS binding to hCB(2) CHO and mouse spleen membranes. THCV (0.3 or 1 mg.kg(-1) i.p.) decreased carrageenan-induced oedema in a manner that seemed to be CB(2) receptor-mediated and suppressed carrageenan-induced hyperalgesia. THCV (i.p.) also decreased pain behaviour in phase 2 of the formalin test at 1 mg.kg(-1), and in both phases of this test at 5 mg.kg(-1); these effects of THCV appeared to be CB(1) and CB(2) receptor mediated.

CONCLUSIONS AND IMPLICATIONS

THCV can activate CB(2) receptors in vitro and decrease signs of inflammation and inflammatory pain in mice partly via CB(1) and/or CB(2) receptor activation.

Authors+Show Affiliations

Institute of Medical Sciences, University of Aberdeen, Aberdeen, UK.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo 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, N.I.H., Extramural
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20590571

Citation

Bolognini, Daniele, et al. "The Plant Cannabinoid Delta9-tetrahydrocannabivarin Can Decrease Signs of Inflammation and Inflammatory Pain in Mice." British Journal of Pharmacology, vol. 160, no. 3, 2010, pp. 677-87.
Bolognini D, Costa B, Maione S, et al. The plant cannabinoid Delta9-tetrahydrocannabivarin can decrease signs of inflammation and inflammatory pain in mice. Br J Pharmacol. 2010;160(3):677-87.
Bolognini, D., Costa, B., Maione, S., Comelli, F., Marini, P., Di Marzo, V., ... Pertwee, R. G. (2010). The plant cannabinoid Delta9-tetrahydrocannabivarin can decrease signs of inflammation and inflammatory pain in mice. British Journal of Pharmacology, 160(3), pp. 677-87. doi:10.1111/j.1476-5381.2010.00756.x.
Bolognini D, et al. The Plant Cannabinoid Delta9-tetrahydrocannabivarin Can Decrease Signs of Inflammation and Inflammatory Pain in Mice. Br J Pharmacol. 2010;160(3):677-87. PubMed PMID: 20590571.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The plant cannabinoid Delta9-tetrahydrocannabivarin can decrease signs of inflammation and inflammatory pain in mice. AU - Bolognini,Daniele, AU - Costa,Barbara, AU - Maione,Sabatino, AU - Comelli,Francesca, AU - Marini,Pietro, AU - Di Marzo,Vincenzo, AU - Parolaro,Daniela, AU - Ross,Ruth A, AU - Gauson,Lisa A, AU - Cascio,Maria G, AU - Pertwee,Roger G, PY - 2010/7/2/entrez PY - 2010/7/2/pubmed PY - 2010/10/15/medline SP - 677 EP - 87 JF - British journal of pharmacology JO - Br. J. Pharmacol. VL - 160 IS - 3 N2 - BACKGROUND AND PURPOSE: The phytocannabinoid, Delta(9)-tetrahydrocannabivarin (THCV), can block cannabinoid CB(1) receptors. This investigation explored its ability to activate CB(2) receptors, there being evidence that combined CB(2) activation/CB(1) blockade would ameliorate certain disorders. EXPERIMENTAL APPROACH: We tested the ability of THCV to activate CB(2) receptors by determining whether: (i) it inhibited forskolin-stimulated cyclic AMP production by Chinese hamster ovary (CHO) cells transfected with human CB(2) (hCB(2)) receptors; (ii) it stimulated [(35)S]GTPgammaS binding to hCB(2) CHO cell and mouse spleen membranes; (iii) it attenuated signs of inflammation/hyperalgesia induced in mouse hind paws by intraplantar injection of carrageenan or formalin; and (iv) any such anti-inflammatory or anti-hyperalgesic effects were blocked by a CB(1) or CB(2) receptor antagonist. KEY RESULTS: THCV inhibited cyclic AMP production by hCB(2) CHO cells (EC(50)= 38 nM), but not by hCB(1) or untransfected CHO cells or by hCB(2) CHO cells pre-incubated with pertussis toxin (100 ng.mL(-1)) and stimulated [(35)S]GTPgammaS binding to hCB(2) CHO and mouse spleen membranes. THCV (0.3 or 1 mg.kg(-1) i.p.) decreased carrageenan-induced oedema in a manner that seemed to be CB(2) receptor-mediated and suppressed carrageenan-induced hyperalgesia. THCV (i.p.) also decreased pain behaviour in phase 2 of the formalin test at 1 mg.kg(-1), and in both phases of this test at 5 mg.kg(-1); these effects of THCV appeared to be CB(1) and CB(2) receptor mediated. CONCLUSIONS AND IMPLICATIONS: THCV can activate CB(2) receptors in vitro and decrease signs of inflammation and inflammatory pain in mice partly via CB(1) and/or CB(2) receptor activation. SN - 1476-5381 UR - https://www.unboundmedicine.com/medline/citation/20590571/The_plant_cannabinoid_Delta9_tetrahydrocannabivarin_can_decrease_signs_of_inflammation_and_inflammatory_pain_in_mice_ L2 - https://doi.org/10.1111/j.1476-5381.2010.00756.x DB - PRIME DP - Unbound Medicine ER -