Interaction of a new potent anticholinesterasic compound (±)huprine X with muscarinic receptors in rat brain

S. Roman, N. M. Vivas, A. Badia, M. V. Clos

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26 Citations (Scopus)

Abstract

The interaction of rac-12-amine-3-clor-6,7,10,11-tetrahydro-9-ethyl-7-11-methanecyclo- octane[b]quinoline ((±)huprine X) with M1 and M2 receptors has been studied in rat brain. Specific binding of [3H]pirenzepine or [3H]quinuclinidylbenzylate to hippocampus preparations was inhibited by (±)huprine X. This drug displayed a greater affinity for M1 (Ki=0.338±0.41 μM) than M2 (Ki=4.66±0.32 μM) receptors. In functional studies, (±)huprine X (1 μM) increased the release of [3H]dopamine in cortical synaptosomes, and this effect was partially reverted by atropine and mecamylamine, suggesting an agonistic effect on both M1 and nicotinic receptors. The inhibitory effect of (±)huprine X (10 μM) on [3H]acetylcholine release and the subsequent reversion by atropine suggests that the drug also has an agonist effect on M2 receptors. The present results demonstrate that this acetylcholinesterase inhibitor has an ample cholinergic profile, which suggests a potential source of interest of (±)huprine X in Alzheimer's disease therapy. © 2002 Elsevier Science Ireland Ltd. All rights reserved.
Original languageEnglish
Pages (from-to)103-106
JournalNeuroscience Letters
Volume325
DOIs
Publication statusPublished - 7 Jun 2002

Keywords

  • Acetylcholinesterase inhibitor
  • Alzheimer's disease
  • Muscarinic receptors
  • Nicotinic receptors

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