Journal article
Gabapentin inhibits presynaptic Ca 2+ influx and synaptic transmission in rat hippocampus and neocortex
European journal of pharmacology, v 449(3)
2002
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
Gabapentin is a widely used drug with anticonvulsant, antinociceptive and anxiolytic properties. Although it has been previously shown that Gabapentin binds with high affinity to the α
2δ subunit of voltage-operated Ca
2+ channels (VOCC), little is known about the functional consequences of this interaction. Here, we investigated the effect of Gabapentin on VOCCs and synaptic transmission in rat hippocampus and neocortex using whole-cell patch clamp and confocal imaging techniques. Gabapentin (100–300 μM) did not affect the peak amplitude or voltage-dependency of VOCC currents recorded from either dissociated or in situ neocortical and hippocampal pyramidal cells. In contrast, Gabapentin inhibited K
+-evoked increases in [Ca
2+] in a subset of synaptosomes isolated from rat hippocampus and neocortex in a dose-dependent manner, with an apparent half-maximal inhibitory effect at ∼100 nM. In hippocampal slices, Gabapentin (300 μM) inhibited the amplitude of evoked excitatory- and inhibitory postsynaptic currents recorded from CA1 pyramidal cells by 30–40%. Taken together, the results suggest that Gabapentin selectively inhibits Ca
2+ influx by inhibiting VOCCs in a subset of excitatory and inhibitory presynaptic terminals, thereby attenuating synaptic transmission.
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Details
- Title
- Gabapentin inhibits presynaptic Ca 2+ influx and synaptic transmission in rat hippocampus and neocortex
- Creators
- Johannes A van Hooft - University of AmsterdamJohn J Dougherty - Hahnemann University HospitalDuco Endeman - University of AmsterdamRobert A Nichols - Hahnemann University HospitalWytse J Wadman - University of Amsterdam
- Publication Details
- European journal of pharmacology, v 449(3)
- Publisher
- Elsevier
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Obstetrics and Gynecology
- Web of Science ID
- WOS:000177679400004
- Scopus ID
- 2-s2.0-0037047706
- Other Identifier
- 991019350599104721
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- Collaboration types
- Domestic collaboration
- International collaboration
- Web of Science research areas
- Pharmacology & Pharmacy