Anticonvulsant properties of linalool in glutamate-related seizure models.
In order to investigate the pharmacodynamic basis of the previously-established anticonvulsant properties of linalool, we examined the effects of this compound on behavioral and neurochemical aspects of glutamate expression in experimental seizure models. Specifically, linalool effects were investigated to determine its inhibition of (i) L-[3H]glutamate binding at CNS (central nervous system membranes), (ii) N-methyl-D-aspartate (NMDA)-induced convulsions, (iii) quinolinic acid (QUIN)-induced convulsions, and the behavioral and neurochemical correlates of PTZ-kindling. The data indicate that linalool modulates glutamate activation expression in vitro (competitive antagonism of L-[3H]glutamate binding) and in vivo (delayed NMDA convulsions and blockage of QUIN convulsions). Linalool partially inhibited and significantly delayed the behavioral expression of PTZ-kindling, but did not modify the PTZ-kindling-induced increase in L-[3H]glutamate binding.
Elisabetsky
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Departamento de Farmacologia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil. elisasky@vortex.ufrgs.br
Brum
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Souza
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D000080462:Acyclic Monoterpenes; D000818:Animals; D000927:Anticonvulsants / Q000494:pharmacology*; D002540:Cerebral Cortex / Q000187:drug effects; D004195:Disease Models, Animal; D016291:Dizocilpine Maleate / Q000494:pharmacology; D018698:Glutamic Acid / Q000378:metabolism / Q000633:toxicity*; D007696:Kindling, Neurologic / Q000187:drug effects; D008297:Male; D039821:Monoterpenes; D016202:N-Methylaspartate / Q000633:toxicity; D010433:Pentylenetetrazole / Q000494:pharmacology; D010634:Phenobarbital / Q000494:pharmacology; D017378:Quinolinic Acid / Q000633:toxicity; D011869:Radioligand Assay; D051381:Rats; D017208:Rats, Wistar; D012640:Seizures / Q000139:chemically induced / Q000517:prevention & control*; D013729:Terpenes / Q000494:pharmacology*
D000080462:Acyclic Monoterpenes; D000927:Anticonvulsants; D039821:Monoterpenes; D013729:Terpenes; D018698:Glutamic Acid; D016202:N-Methylaspartate; D016291:Dizocilpine Maleate; C018584:linalool; D017378:Quinolinic Acid; D010433:Pentylenetetrazole; D010634:Phenobarbital