期刊
CHANNELS
卷 4, 期 6, 页码 490-496出版社
LANDES BIOSCIENCE
DOI: 10.4161/chan.4.6.12864
关键词
gabapentin; pregabalin; calcium channels; synaptic transmission; neuromuscular junction; calyx of Held; mice
资金
- UBACYT [X-223]
- PICT [BID 1728 OC.AR.PICT 2005 N 32113]
- FONCYT (ANPCyT) PICT [BID 1728 OC.AR.PICT 2006 N 199, PIDRI-PRH 2007, 2007-1009]
- Wellcome Trust [084636]
Gabapentin and pregabalin are anticonvulsant drugs that are extensively used for the treatment of several neurological and psychiatric disorders. Gabapentinoids (GBPs) are known to have a high affinity binding to alpha(2)delta-1 and alpha(2)delta-2 auxiliary subunit of specific voltage-gated calcium channels. Despite the confusing effects reported on Ca(2+) currents, most of the studies showed that GBPs reduced release of various neurotransmitters from synapses in several neuronal tissues. We showed that acute in vitro application of pregabalin could reduce in a dose dependent manner synaptic transmission in both neuromuscular junctions and calyx of Held-MNTB excitatory synapses. Furthermore presynaptic Ca2+ currents treated with pregabalin are reduced in amplitude, do not show inactivation at a clinically relevant low concentration of 100 mu M and activate and deactive faster. These results suggest novel modulatory role of acute pregabalin that might contribute to better understanding its anticonvulsant/analgesic clinical effects.
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