Abstract:
:Blockade of sodium channels located in the sinoatrial node can slow diastolic depolarisation rate, recorded in vitro. The objective was therefore to determine whether these blockers could slow heart rate in vivo. The heart rate was firstly measured in spontaneously beating, isolated rat heart atria in the presence of different voltage gated sodium channel blockers. Tetrodotoxin and lidocaine slightly reduced heart rate whereas KC 12291 and R 56865, which mainly interact with the persistent component of the sodium current, concentration dependently and potently induced bradycardia. In the pithed rat, tetrodotoxin induced statistically significant decreases heart rate, maximal effects were: -32.2+/-6.1 beat per min. KC 12291 and R 56865 dose-dependently induced bradycardia (Delta heart rate obtained, -55.1+/-5.2 beat per min, P<0.05, and -71.9+/-8.5 bpm, P<0.05, respectively). In conclusion, voltage gated sodium channel blockers rather selective for the persistent current, exert a potent bradycardic effect in the rat.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Létienne R,Vié B,Le Grand Bdoi
10.1016/j.ejphar.2005.11.035keywords:
subject
Has Abstractpub_date
2006-01-20 00:00:00pages
243-9issue
3eissn
0014-2999issn
1879-0712pii
S0014-2999(05)01221-5journal_volume
530pub_type
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