Lestaurtinib (CEP-701) attenuates "second hit" kainic acid-induced seizures following early life hypoxic seizures

Epilepsy Res. 2014 May;108(4):806-10. doi: 10.1016/j.eplepsyres.2014.01.019. Epub 2014 Jan 31.

Abstract

Tropomyosin-related kinase receptor B (TrkB) activation has been implicated in epileptogenesis. We investigated hippocampal levels of phosphorylated TrkB (p-TrkB) and potential antiepileptogenic actions of the tyrosine kinase inhibitor, lestaurtinib (CEP-701) in postnatal day 10 (P10) rat pups following hypoxic seizures (HS). Hippocampal expression of p-TrkB over total TrkB protein levels were assessed by immunoblot at 6, 12, or 24 h post-HS, and revealed a statistically significant and transient 1.5-fold increase in hippocampal p-TrkB 12 h post-HS compared to littermate normoxic controls. To investigate the effects of CEP-701, pups were treated with 2 doses of CEP-701 intraperitoneally (i.p.), 3 mg/kg/dose, immediately after and 12 h post-HS. P-TrkB levels and susceptibility to kainic acid (KA)-induced seizures at P14 were compared between post-HS CEP-701-treated pups, post-HS vehicle-treated pups and normoxic littermates. Post-treatment with CEP-701 reversed the increased TrkB phosphorylation to baseline normoxic levels and attenuated the HS-related enhanced susceptibility to KA-induced seizures at P14. Given its known clinical safety profile, CEP-701 is a promising clinically translatable therapy to prevent epileptogenesis in the immature brain.

Keywords: Epileptogenesis; Hypoxic seizures; Memory; Neonates; Tropomyosin-related kinase receptor; Tyrosine kinase receptor.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Anticonvulsants / pharmacology
  • Anticonvulsants / therapeutic use*
  • Carbazoles / pharmacology
  • Carbazoles / therapeutic use*
  • Furans
  • Hippocampus / drug effects*
  • Hippocampus / metabolism
  • Hypoxia / complications*
  • Hypoxia / metabolism
  • Kainic Acid
  • Male
  • Phosphorylation
  • Rats
  • Rats, Long-Evans
  • Receptor, trkB / metabolism*
  • Seizures / chemically induced
  • Seizures / drug therapy*
  • Seizures / metabolism

Substances

  • Anticonvulsants
  • Carbazoles
  • Furans
  • lestaurtinib
  • Receptor, trkB
  • Kainic Acid