Riluzole, a novel antiglutamate, blocks GABA uptake by striatal synaptosomes.
The effect of riluzole (2-amino-6-trifluoro-methoxybenzothiazole, a novel antiglutamate agent) on the uptake of [3H]GABA (gamma-aminobutyric acid) by striatal synaptosomes was investigated in rats. Both nipecotic acid (a classical blocker of GABA uptake) and riluzole were found to inhibit [3H]GABA uptake in a dose-related fashion (IC50 = 3.6 x 10(-6) M and 4.3 x 10(-5) M for nipecotic acid and riluzole, respectively). These results indicate that, in addition to its antiglutamate properties, riluzole probably also promotes synaptic GABA accumulation, which might contribute to the anticonvulsant and/or anesthetic properties of this pharmacological agent.
Mantz
J
J
Department of Anesthesiology, Hospital Bichat, Paris, France.
Laudenbach
V
V
Lecharny
J B
JB
Henzel
D
D
Desmonts
J M
JM
D000818:Animals; D003342:Corpus Striatum / Q000187:drug effects* / Q000378:metabolism; D018691:Excitatory Amino Acid Antagonists; D018756:GABA Antagonists; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D019782:Riluzole; D013574:Synaptosomes / Q000187:drug effects* / Q000378:metabolism; D013844:Thiazoles / Q000008:administration & dosage / Q000494:pharmacology*
D018691:Excitatory Amino Acid Antagonists; D018756:GABA Antagonists; D013844:Thiazoles; D019782:Riluzole