The action of pyrantel as an agonist and an open channel blocker at acetylcholine receptors in isolated Ascaris suum muscle vesicles

European Journal of Pharmacology
S J RobertsonR J Martin

Abstract

The anthelmintic pyrantel is believed to act as an agonist at acetylcholine receptors on somatic muscle from the parasite Ascaris suum. This study aimed to confirm this mode of action of pyrantel. Single-channel recordings from muscle vesicles formed from the extrasynaptic region of the bag of somatic muscle cells of Ascaris suum were made using the patch-clamp technique. Pyrantel (0.03-100 microM) activated cation-selective channels with at least 2 conductance levels: main conductance 41 +/- 2.04 pS (mean +/- S.E., n = 28), smaller conductance 22.4 +/- 0.34 pS (mean +/- S.E., n = 8). The current/voltage plots showed a linear relationship. Detailed kinetic analysis revealed that activation of the receptor by pyrantel resulted in at least 2 distinct open and burst states and at least 3 distinct closed states. The mean open time of the channel, with 0.1 microM pyrantel, was 1.53 +/- 0.22 ms (mean +/- S.E., n = 7) at -75 mV. We have previously shown that acetylcholine activated channels with similar properties to the pyrantel-activated channels (Pennington, A.J. and R.J. Martin, 1990, J. Exp. Biol. 154, 201) confirming that pyrantel is an acetylcholine agonist. With high concentrations (100 microM) of pyrantel a sequence of rapid ...Continue Reading

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Citations

Nov 14, 2007·Invertebrate Neuroscience : in·Alan P Robertson, Richard J Martin
Jun 14, 2005·International Journal for Parasitology·Mark M LevandoskiRichard J Martin
Jun 18, 2003·European Journal of Pharmacology·Mark M LevandoskiJane Chang
Jul 23, 1998·International Journal for Parasitology·R J MartinN Sangster
Dec 24, 1997·Brain Research. Brain Research Reviews·H R Arias
Jan 1, 1996·Parasitology·R J MartinI Murray
Jan 13, 2010·Molecular and Biochemical Parasitology·Sreekanth PuttacharyRichard J Martin
Aug 28, 2007·The Veterinary Journal·Steven R KoppGlen T Coleman
Jan 22, 2008·International Journal for Parasitology·Sasa M TrailovicRichard J Martin
Jul 16, 2008·Biochimica Et Biophysica Acta·Ana Sofía VallésFrancisco J Barrantes
May 6, 2014·Frontiers in Physiology·Timothy Lynagh, Stephan A Pless
Jun 16, 2016·Journal of Veterinary Pharmacology and Therapeutics·J H WhittakerM T Brewer
Mar 31, 2009·International Journal for Parasitology·Michael J KimberPaula Ribeiro
Jul 17, 2003·Journal of Postgraduate Medicine·R ParedesB Clotet
Apr 15, 2017·Behavioural Neurology·Jennifer A FoleyLisa Cipolotti
Mar 1, 2021·European Journal of Pharmacology·Takashi OkudaHidemi Misawa
Feb 9, 2018·Acta veterinaria·Melanie AbongwaAlan P Robertson
Mar 23, 2001·Journal of Medicinal Chemistry·P T Meinke

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