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Anticholinergic potency of psychoactive drugs in human and rat cerebral cortex and striatum

Academic Article
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Overview

authors

  • Danielsson, E.
  • Peterson, L. L.
  • Grundin, R.
  • Ogren, S. O.
  • Bartfai, Tamas

publication date

  • 1985

journal

  • Life Sciences  Journal

abstract

  • The affinity of selected antipsychotic and antidepressant drugs for the muscarinic receptor was studied in membranes from both human and rat striatum and cerebral cortex. While there are regional differences in the anticholinergic potency of the drugs, there is good agreement between the obtained inhibition constants from the corresponding human and rat striatum (r: 0.98) and from human and rat cerebral cortex (r: 0.96). There is also good agreement between the obtained Ki values within one species: human cerebral cortex versus human striatum (r: 0.99) and for rat cerebral cortex and rat striatum (r: 0.87). Thus, the previously published quantitative estimates of the antimuscarinic activity of psychoactive drugs which were derived from studies on membranes from rat brain give an accurate estimate of the antimuscarinic activity in human brain. The drugs tested in this study include chlorpromazine acetophenazine, haloperidol, sulpiride, remoxipride (FLA-731 (-), a substituted benzamide), amitriptyline and two serotonin uptake blockers: norzimelidine and alaproclate.

subject areas

  • Aged
  • Animals
  • Antidepressive Agents
  • Antipsychotic Agents
  • Benzilates
  • Cerebral Cortex
  • Corpus Striatum
  • Humans
  • In Vitro Techniques
  • Male
  • Parasympatholytics
  • Piperidines
  • Psychotropic Drugs
  • Rats
  • Rats, Inbred Strains
  • Receptors, Muscarinic
  • Species Specificity
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Identity

International Standard Serial Number (ISSN)

  • 0024-3205

Digital Object Identifier (DOI)

  • 10.1016/0024-3205(85)90052-9

PubMed ID

  • 2858803
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Additional Document Info

start page

  • 1451

end page

  • 1457

volume

  • 36

issue

  • 15

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