Mechanism responsible for epileptogenic activity by first-generation H1-antagonists in rats

Chiaki Kamei, Masaya Ohuchi, Yukio Sugimoto, Chihiro Okuma

Research output: Contribution to journalArticlepeer-review

48 Citations (Scopus)


In the present study, we have demonstrated that multiple first-generation H1-antagonists caused behavioral and EEG seizures in rats. The epileptogenic property of pyrilamine was more potent than either chlorpheniramine or diphenhydramine. In contrast, the second-generation H1-antagonists, loratadine and ebastine did not induce detectable epileptogenic activity. Intraperitoneal injection of histidine inhibited the EEG seizures induced by pyrilamine, diphenhydramine or chlorpheniramine; however no antagonism was observed with physostigmine. These results clearly suggest that the epileptogenic activity of first-generation H1-antagonists is dependent upon a centrally acting histaminergic mechanism.

Original languageEnglish
Pages (from-to)183-186
Number of pages4
JournalBrain Research
Issue number1
Publication statusPublished - Dec 22 2000


  • Chlorpheniramine
  • Diphenhydramine
  • Epileptogenic activity
  • Histidine
  • Physostigmine
  • Pyrilamine

ASJC Scopus subject areas

  • Neuroscience(all)
  • Molecular Biology
  • Clinical Neurology
  • Developmental Biology


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