The effect of haloperidol on the histaminergic neuron system in the rat brain

Chihiro Ito, Kenji Onodera, Atsushi Yamatodani, Kazuhiko Yanai, Eiko Sakurai, Mitsumoto Sato, Takehiko Watanabe

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)


In this study, the effect of haloperidol on histamine (HA) levels, histidine decarboxylase (HDC) activities and the bindings of [3H]-(R)-α- methyhistamine ([3H]-(R)-α-MeHA) to histamine H3 receptors were investigated in the rat brain. Administration of 10 mg/kg of haloperidol decreased HA levels in the rat striatum and diencephalon, but increased HDC activities in rat striatum and diencephalon, although that of 5 mg/kg did not change them. Meanwhile, haloperidol inhibited the bindings of [3H]-(R)-α- MeHA to H3 receptor sites in the rat striatal membrane with a Ki value of 10.5 + 0.45 μM. These findings suggest that only a high dose of haloperidol increases HA synthesis and release as a histamine H3 receptor antagonist in the rat brain.

Original languageEnglish
Pages (from-to)285-292
Number of pages8
JournalTohoku Journal of Experimental Medicine
Issue number4
Publication statusPublished - 1997 Dec


  • Haloperidol
  • Histamine H receptor
  • Histamine level
  • Histidine decarboxylase
  • Rat brain


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