Nicergoline Enhances Glutamate Uptake via Glutamate Transporters in Rat Cortical Synaptosomes

To elucidate the mechanisms of neuroprotective action of nicergoline, we examined its effect on glutamate transport in rat cortical synaptosomes and cloned glutamate transporters. In synaptosomes, nicergoline enhanced the glutamate uptake at 1—10 μM in standard medium and suppressed the increase of...

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Bibliographic Details
Published in:Biological & pharmaceutical bulletin 2004, Vol.27(6), pp.817-820
Main Authors: Nishida, Atsushi, Iwata, Hiroshi, Kudo, Yukitsuka, Kobayashi, Tsutomu, Matsuoka, Yuzo, Kanai, Yoshikatsu, Endou, Hitoshi
Format: Article
Language:English
Subjects:
Amino Acid Transport System X-AG - metabolism
Animals
Cerebral Cortex - drug effects
Cerebral Cortex - metabolism
Dose-Response Relationship, Drug
Female
glutamate reversed transport
glutamate transporter
glutamate uptake
Glutamic Acid - metabolism
Male
nicergoline
Nicergoline - pharmacology
Rats
Rats, Wistar
synaptosome
Synaptosomes - drug effects
Synaptosomes - metabolism
Xenopus laevis
Xenopus oocyte
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Summary:To elucidate the mechanisms of neuroprotective action of nicergoline, we examined its effect on glutamate transport in rat cortical synaptosomes and cloned glutamate transporters. In synaptosomes, nicergoline enhanced the glutamate uptake at 1—10 μM in standard medium and suppressed the increase of extracellular glutamate by reversed transport in low Na+ medium. Apparent increase of extracellular glutamate concentration by dihydrokinate, an inhibitor of glial glutamate transporter GLT-1, was antagonized by nicergoline. In Xenopus oocytes expressing mouse neuronal glutamate transporter (mEAAC1), the glutamate-induced inward current was enhanced by nicergoline. These results suggest that nicergoline reduces the extracellular glutamate concentration through its effect on glutamate transporters.
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.27.817