Choline high-affinity uptake and metabolism and choline acetyltransferase activity in the striatum of rats chronically treated with neuroleptics

J Neurochem. 1980 Sep;35(3):606-11. doi: 10.1111/j.1471-4159.1980.tb03698.x.


High-affinity uptake of choline and choline acetyltransferase activity (ChAT) were measured in the striatum of rats treated for 45-60 days with haloperidol (1 mg/kg per os) and pimozide (1 mg/kg per os) daily and with fluspirilene (1 mg/kg i.m.) twice a week. Haloperidol and fluspirilene caused a 20%, and pimozide a 38%, increase in high-affinity uptake of choline. They also caused a significant decrease in ChAT activity: haloperidol, 20%; pimozide, 27%; and fluspirilene, 42%. In rats treated with fluspirilene for 65-80 days the metabolism of [3H] choline taken up by striatal synaptosomes was investigated. A 33% increase in total radioactivity, a significant increase in labelled acetylcholine (ACh), a relative decrease in labelled choline, and no change in labelled phosphorylcholine and betaine were found. It is concluded that the increase in high-affinity choline uptake caused by chronic administration of neuroleptic drugs is associated with a parallel increase in choline utilization for ACh formation. On the other hand, the decrease in ChAT activity does not appear to influence ACh formation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antipsychotic Agents / pharmacology*
  • Choline / metabolism*
  • Choline O-Acetyltransferase / metabolism*
  • Corpus Striatum / drug effects
  • Corpus Striatum / metabolism*
  • Fluspirilene / pharmacology
  • Haloperidol / pharmacology
  • In Vitro Techniques
  • Male
  • Pimozide / pharmacology
  • Rats
  • Synaptosomes / metabolism
  • Time Factors


  • Antipsychotic Agents
  • Pimozide
  • Fluspirilene
  • Choline O-Acetyltransferase
  • Haloperidol
  • Choline