Muscarinic subtype selectivity of tetrahydroaminoacridine: Possible relationship to its capricious efficacy

Jennifer S. Kiefer-Day, Hope E. Campbell, Joseph Towles, Esam E. El-Fakahany

Research output: Contribution to journalArticlepeer-review

17 Scopus citations

Abstract

Tetrahydroaminoacridinc discriminated slightly in its potency to displace [3H]N-methylscopolamine ([3H]NMS) binding from different muscarinic receptor subtypes (M2 > M1 > M3) and to allosterically decelerate ligand binding (M2 ≥ M1 > M3). T steep displacement curves suggest that marked changes in receptor occupancy may occur within a relatively narrow dose range. Thus, individual inter-patient variability and inconsistent results in clinical studies may be related to blockade of muscarinic receptors, which would oppose the beneficial effects resulting from acetylcholinesterase inhibition.

Original languageEnglish (US)
Pages (from-to)421-423
Number of pages3
JournalEuropean Journal of Pharmacology
Volume203
Issue number3
DOIs
StatePublished - Oct 22 1991

Bibliographical note

Funding Information:
This studyw as supportedi n part by Grants NS2S743a nd AG-07118f rom the National Institutes of Health and by Contract DAAL-03-K-88-0078 from the U.S. Army Research Office. J. S. K. was a recipient of an Emerson FelIowship from the Universityo f Marylandd uringthe courseo f this work. E. E. E. is a recipiento f a ResearchC areer Development Award from the National fnstitutes of Health (AC-00344). The authors would like to thankM ike Gentry for his excellent technical assistance.

Copyright:
Copyright 2014 Elsevier B.V., All rights reserved.

Keywords

  • (Rat)
  • Allosteric antagonists
  • Brain
  • Muscarinic receptor subtypes
  • Muscarinic receptors
  • Tetrahydroaminoacridine

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