Muscarinic cholinergic receptors in human narcolepsy: a PET study

Neurology. 1998 Nov;51(5):1297-302. doi: 10.1212/wnl.51.5.1297.

Abstract

Objectives: To investigate the function of the muscarinic cholinergic receptor (mAchR) in narcolepsy and the effects of pharmacotherapy on mAchRs.

Background: Muscarinic neural transmission serves as the main executive system in REM sleep. Studies in canine narcolepsy reported an increase in mAchRs in the pons.

Methods: The mAchRs of 11 drug naive/free patients with narcolepsy and 21 normal controls were investigated using PET with [11C]N-methyl-4-piperidylbenzilate ([11C]NMPB). Measurements were done in the pons, thalamus, striatum, and cerebral cortex. Seven of the 11 patients also underwent additional PET scans after the alleviation of symptoms by pharmacotherapy.

Results: There were no differences in [11C]NMPB binding between the control and drug naive/free patients in all areas analyzed. At the time of on-medication PET scan, [11C]NMPB binding in the thalamus was decreased, but only to a small degree compared with that by anticholinergic drugs.

Conclusion: The present results do not support the notion that the mAchR is the main site of action of pharmacotherapy in the marked clinical improvement of human cataplexy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Animals
  • Benzilates / pharmacokinetics
  • Brain / diagnostic imaging
  • Brain / metabolism*
  • Carbon Radioisotopes / pharmacokinetics
  • Central Nervous System Agents / blood
  • Central Nervous System Agents / therapeutic use
  • Dogs
  • Humans
  • Male
  • Narcolepsy / diagnostic imaging*
  • Narcolepsy / drug therapy
  • Narcolepsy / metabolism*
  • Organ Specificity
  • Parasympatholytics / pharmacokinetics
  • Piperidines / pharmacokinetics
  • Receptors, Muscarinic / analysis*
  • Reference Values
  • Regression Analysis
  • Tomography, Emission-Computed

Substances

  • Benzilates
  • Carbon Radioisotopes
  • Central Nervous System Agents
  • Parasympatholytics
  • Piperidines
  • Receptors, Muscarinic
  • mepenzolic acid