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Comparative effects of ultra-short-acting beta1-blockers on voltage-gated tetrodotoxin-resistant Na+ channels in rat sensory neurons

BACKGROUND AND OBJECTIVE: To examine a possible mechanism for their antinociceptive actions, we compared the effects of two clinically used ultra-short-acting beta1-blockers, landiolol and esmolol, on tetrodotoxin-resistant sodium (TTX-r Na) channels in rat dorsal root ganglion neurons, which are important for nociception. METHODS: In small (<30 microm) dorsal root ganglion neurons from Sprague-Dawley rats, recordings of whole-cell membrane currents were made using the patch-clamp technique. To examine the effects of landiolol and esmolol on TTX-r Na currents, whole-cell membrane Na currents were evoked every 10 s by stepping for 50 ms from a holding potential of -70 to -10 mV. Each drug was applied at stepwise-increased concentrations every 2 min. The voltage dependence of the steady-state inactivation of the TTX-r Na current was investigated by using a conventional double-pulse protocol. To test for use-dependent blockade of TTX-r Na channels by beta-blockers, trains of depolarizing pulses (to -10 from a holding potential of -70 mV) were applied at one of three frequencies (0.2, 5 or 20 Hz) in the absence or presence of drug (landiolol 8 mmol l, esmolol 140 micromol l). RESULTS: Esmolol blocked TTX-r Na currents in a dose-dependent and use-dependent manner, but a very high concentration of landiolol was required to block TTX-r Na channel activities. The half-maximal inhibitory concentrations (IC50) for the TTX-r Na current were (holding potential, -70 mV) landiolol 7.66 +/- 0.62 mmol l (n = 6) and esmolol 145 +/- 7.5 micromol l (n = 6), and the Hill coefficients were landiolol 1.06 +/- 0.09 (n = 6) and esmolol 0.96 +/- 0.05 (n = 6). CONCLUSION: Esmolol, but not landiolol, may have useful effects against pain related to TTX-r Na channel activity Keywords : Adrenergic beta-Antagonists,analogs & derivatives,Animals,drug effects,Drug Resistance,Electrophysiological Phenomena,Ion Channel Gating,Kinetics,Male,metabolism,methods,Morpholines,Neurons,Pain,Patch-Clamp Techniques,pharmacology,Propanolamines,Rats,Rats,Sprague-Dawley,Sensory Receptor Cells,Sodium Channels,Tetrodotoxin,Time Factors,Urea,, Effects,Ultrashortacting,Beta1blockers, best clinics in london

Date of Publication : 2009 Mar

Authors : Tanahashi S;Iida H;Dohi S;Oda A;Osawa Y;Yamaguchi S;

Organisation : Department of Anesthesiology and Pain Medicine, Gifu University School of Medicine, Gifu city, Japan. rushex7775@yahoo.co.jp

Journal of Publication : Eur J Anaesthesiol

Pubmed Link : https://www.ncbi.nlm.nih.gov/pubmed/19237982

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Comparative effects of ultra-short-acting beta1-blockers on voltage-gated tetrodotoxin-resistant Na+ channels in rat sensory neurons | Harley street orthopaedic surgeons

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