Instituut voor Neuropathische Pijn
English articles Gliopathic pain Palmitoylethanolamide analogue, palmitoylallylamide (L-29) in a pain model
| Palmitoylethanolamide analogue, palmitoylallylamide (L-29) in a pain model |
|
Cannabis and the endogenous cannabinoids are associated with analgesia in acute and chronic pain states. The analgesic effect of the palmitoylethanolamide (PEA) has ben described in many different animal models, and meanhile also in a number of clinical trials. This has prompted to look for analogues of PEA. Palmitoylallylamide (L-29) is such a analogue.
Systemically administered L-29 (10 mg kg(-1)) reduced hypersensitivity to mechanical and thermal stimuli in the partial sciatic nerve injury (PSNI) model of neuropathic pain; and mechanical hypersensitivity in a model of antiretroviral (ddC)-associated hypersensitivity and a model of varicella zoster virus (VZV)-associated hypersensitivity. L-29's activity is comparable to palmitoylethanolamide itself and works within the same concentration range. L-29 analgesic effects were comparable to those of gabapentin (50 mg kg(-1)). The analgesic effects could be reduced by administrating the CB(1) receptor antagonist SR141716a (1 mg kg(-1)) ans well as by the CB(2) receptor antagonist SR144528 (1 mg kg(-1)) in the first pain model. The analgesic effects could be partly reduced by the peroxisome proliferator-activated receptor-alpha antagonist, MK-886 (1 mg kg(-1)). The conclusion was: L-29 produces analgesia in a range of neuropathic pain models. This presents L-29 as a novel analgesic compound that may target the endogenous cannabinoid system while avoiding undesirable side effects associated with direct cannabinoid receptor activation. [1] Jan M. Keppel Hesselink, MD, PhD, January 2011 Referenties[1]: Wallace VC, Segerdahl AR, Lambert DM, Vandevoorde S, Blackbeard J, Pheby T, Hasnie F, Rice AS. | The effect of the palmitoylethanolamide analogue, palmitoylallylamide (L-29) on pain behaviour in rodent models of neuropathy. | Br J Pharmacol. | 2007 Aug;151(7):1117-28. Epub 2007 Jun 11. |