Nicergoline enhances glutamate uptake via glutamate transporters in rat cortical synaptosomes
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Updated: Aug 24, 2026

Methodology for Biomimetic Chemical Neuromodulation of Rat Retinas with the Neurotransmitter Glutamate In Vitro
Published on: December 19, 2017
Atsushi Nishida1, Hiroshi Iwata, Yukitsuka Kudo
1Discovery and Pharmacology Research Laboratories, Tanabe Seiyaku Co., Ltd., Toda, Saitama, Japan. bon@tanabe.co.jp
Abstract:
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 microM 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.
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