Summary:Purpose: The purpose of this study was to evaluate in mice the anticonvulsant potential of N-palmitoylethanolamide, a putative endocannabinoid that accumulates in the body during inflammatory processes.Methods: N-palmitoylethanolamide was injected intraperitoneally (i.p.) in mice and evaluated for anticonvulsant activity [in maximal electroshock seizure (MES) and chemical-induced convulsions] and for neurologic impairment (rotorod). It was compared with anandamide and with different palmitic acid analogues as well as with reference anticonvulsants (AEDs) injected under the same conditions.Results: The MES test showed, after i.p. administration to mice, that N-palmitoylethanolamide had an median effective dose (ED 50 ) value comparable to that of phenytoin (PHT; 8.9 and 9.2 mg/kg, respectively). In the subcutaneous pentylenetetrazol test and in the 3-mercaptropropionic acid test, it was effective only against tonic convulsions. N-palmitoylethanolamide was devoid of neurologic impairment Յ250 mg/kg, yielding a high protective index.Conclusions: N-palmitoylethanolamide, an endogenous compound with antiinflammatory and analgesic activities, is a potent AED in mice. Its precise mechanism of action remains to be elucidated.
Synthesis of 6-Benzoyl-2(3H)-benzoxazolone and 6-Benzoyl-2(3H) benzothiazolone.-Different methods for the synthesis of the title compounds (IV), interesting analgesic drugs, are reported and compared. The AlCl3-catalyzed migration of the acyl-group from the N-atom to the 6-position proves to be the most effective one. -(UCAR, H.; VAN DERPOORTEN, K.; KANYONYO, M.; ISA, M.; LAMBERT, D.; LESIEUR, D.; POUPAERT, J. H.; Bull.
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