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Archives of Toxicology

, Volume 64, Issue 6, pp 482–489 | Cite as

Bispyridinium (oxime) compounds antagonize the “ganglion blocking” effect of pyridostigmine in isolated superior cervical ganglia of the rat

  • Christel Schlagmann
  • Hanna Ulbrich
  • Jörg Remien
Article

Abstract

The “antidotal effectiveness” of several bispyridinium compounds (HGG 12, HGG 65, HGG 70, HI 6, HLö 7 and HLö 12) against the acetylcholinesterase (AChE) inhibitor pyridostigmine was evaluated in isolated superior cervical ganglia of the rat. Compound action potential amplitudes were inhibited by pyridostigmine in a concentration-dependent manner. HI 6 and atropine proved to be the most effective compounds in antagonizing the “ganglion blocking” action of pyridostigmine. Their relative effectiveness (PE value) was 5.4 and 4.2, respectively. All of the six bispyridinium compounds inhibited carbachol-induced, nicotinic, ganglionic surface depolarizations. The antinicotinic potencies of HI 6 and HLö 7 were about one order of magnitude lower (apparent KI values: 294 and 330 μmol/1) than the antinicotinic potencies of HGG 12, HGG 65, HGG 70 and HLö 12 (apparent KI values ranging from 19 to 41 μmol/1). The antinicotinic potencies of the bispyridinium compounds did not correlate with their in vitro protection of synaptic transmission in sympathetic ganglia. Moreover, the effectiveness of atropine points to the importance of antimuscarinic properties of possible “antidotes” for the maintenance of ganglionic transmission in cases of AChE poisoning.

Key words

Superior cervical ganglion Ganglionic transmission Antinicotinic properties Acetylcholinesterase inhibition Bispyridinium (oxime) compounds Pyridostigmine Physostigmine 

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Copyright information

© Springer-Verlag 1990

Authors and Affiliations

  • Christel Schlagmann
    • 1
  • Hanna Ulbrich
    • 1
  • Jörg Remien
    • 1
  1. 1.Walther Straub-Institut für Pharmakologie und Toxikologie der Ludwig-Maximilians-Universität MünchenMünchen 2Federal Republic of Germany

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