Document Detail


A novel CaV2.2 channel inhibition by piracetam in peripheral and central neurons.
MedLine Citation:
PMID:  23045722     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
No mechanistic actions for piracetam have been documented to support its nootropic effects. Voltage-gated calcium channels have been proposed as a promising pharmacological target of nootropic drugs. In this study, we investigated the effect of piracetam on Ca(V)2.2 channels in peripheral neurons, using patch-clamp recordings from cultured superior cervical ganglion neurons. In addition, we tested if Ca(V)2.2 channel inhibition could be related with the effects of piracetam on central neurons. We found that piracetam inhibited native Ca(V)2.2 channels in superior cervical ganglion neurons in a dose-dependent manner, with an IC(50) of 3.4 μmol/L and a Hill coefficient of 1.1. GDPβS dialysis did not prevent piracetam-induced inhibition of Ca(V)2.2 channels and G-protein-coupled receptor activation by noradrenaline did not occlude the piracetam effect. Piracetam altered the biophysical characteristics of Ca(V)2.2 channel such as facilitation ratio. In hippocampal slices, piracetam and ω-conotoxin GVIA diminished the frequency of excitatory postsynaptic potentials and action potentials. Our results provide evidence of piracetam's actions on Ca(V)2.2 channels in peripheral neurons, which might explain some of its nootropic effects in central neurons.
Authors:
Jorge Bravo-Martínez; Isabel Arenas; Oscar Vivas; Santiago Rebolledo-Antúnez; Mario Vázquez-García; Arturo Larrazolo; David E García
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2012-10-08
Journal Detail:
Title:  Experimental biology and medicine (Maywood, N.J.)     Volume:  237     ISSN:  1535-3699     ISO Abbreviation:  Exp. Biol. Med. (Maywood)     Publication Date:  2012 Oct 
Date Detail:
Created Date:  2012-11-01     Completed Date:  2013-02-05     Revised Date:  2013-09-26    
Medline Journal Info:
Nlm Unique ID:  100973463     Medline TA:  Exp Biol Med (Maywood)     Country:  England    
Other Details:
Languages:  eng     Pagination:  1209-18     Citation Subset:  IM    
Affiliation:
Department of Physiology, School of Medicine, Universidad Nacional Autónoma de México, México, D.F., México.
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MeSH Terms
Descriptor/Qualifier:
Animals
Calcium Channel Blockers / pharmacology*
Calcium Channels, N-Type / metabolism*
Cells, Cultured
Hippocampus / cytology*,  metabolism
Male
Neurons / drug effects*,  metabolism
Nootropic Agents / pharmacology*
Patch-Clamp Techniques
Piracetam / pharmacology*
Rats
Rats, Wistar
Receptors, G-Protein-Coupled / metabolism
Signal Transduction
Superior Cervical Ganglion / cytology*,  metabolism
Chemical
Reg. No./Substance:
0/Calcium Channel Blockers; 0/Calcium Channels, N-Type; 0/Nootropic Agents; 0/Receptors, G-Protein-Coupled; 7491-74-9/Piracetam

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