Ivabradine (a hyperpolarization activated cyclic nucleotide-gated channel blocker) elevates the threshold for maximal electroshock-induced tonic seizures in mice

Pharmacol Rep. 2013;65(5):1407-14. doi: 10.1016/s1734-1140(13)71500-7.

Abstract

Background: The aim of this study was to determine the effect of ivabradine (a hyperpolarization activated cyclic nucleotide-gated channel (HCN) blocker) on the threshold for maximal electroshock (MEST)-induced tonic seizures in mice.

Methods: Electroconvulsionswere produced inmice by means of a current (sine-wave, 50Hz, maximum 500 V, strength from 3-10 mA, ear-clip electrodes, 0.2-s stimulus duration, tonic hindlimb extension taken as the endpoint).

Results: Ivabradine administered intraperitoneally (ip), 60 min before the MEST test, at doses of 5 and 10 mg/kg, did not alter the threshold for maximal electroconvulsions in mice. In contrast, ivabradine at doses of 15 and 20 mg/kg significantly elevated the threshold for maximal electroconvulsions in mice (p < 0.05 and p < 0.001, respectively). Linear regression analysis of ivabradine doses and their corresponding threshold increases allowed determination of the threshold increasing doses by 20 and 50% (TID20 and TID50 values) that elevate the threshold in drug-treated animals over the threshold in control animals. The experimentally derived TID20 and TID50 values for ivabradine were 8.70 and 18.29 mg/kg, respectively.

Conclusions: Based on this preclinical study, one can ascertain that ivabradine dose-dependently increased the threshold for MEST-induced seizures, suggesting the antiseizure activity of the compound in this seizure model in mice.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticonvulsants / administration & dosage
  • Anticonvulsants / pharmacology*
  • Behavior, Animal / drug effects
  • Benzazepines / administration & dosage
  • Benzazepines / pharmacology*
  • Brain / drug effects*
  • Brain / metabolism
  • Brain / physiopathology
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Electroshock*
  • Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels / antagonists & inhibitors*
  • Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels / metabolism
  • Injections, Intraperitoneal
  • Ivabradine
  • Male
  • Memory / drug effects
  • Mice
  • Motor Activity / drug effects
  • Muscle Strength / drug effects
  • Seizures / etiology
  • Seizures / metabolism
  • Seizures / physiopathology
  • Seizures / prevention & control*
  • Seizures / psychology

Substances

  • Anticonvulsants
  • Benzazepines
  • Hyperpolarization-Activated Cyclic Nucleotide-Gated Channels
  • Ivabradine