The effect of the anthelmintic emodepside at the neuromuscular junction of the parasitic nematode Ascaris suum.

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  • Additional Information
    • Source:
      Publisher: Cambridge University Press Country of Publication: England NLM ID: 0401121 Publication Model: Print Cited Medium: Print ISSN: 0031-1820 (Print) Linking ISSN: 00311820 NLM ISO Abbreviation: Parasitology Subsets: MEDLINE
    • Publication Information:
      Original Publication: London, New York, Cambridge University Press.
    • Subject Terms:
      Depsipeptides*; Anthelmintics/*pharmacology ; Ascaris suum/*drug effects ; Neuromuscular Junction/*drug effects ; Peptides, Cyclic/*pharmacology; Acetylcholine/antagonists & inhibitors ; Acetylcholine/pharmacology ; Animals ; Ascaris suum/physiology ; Calcium/metabolism ; Furylfuramide/pharmacology ; In Vitro Techniques ; Muscle Cells/drug effects ; Muscle Cells/physiology ; Muscle Contraction/drug effects ; Muscle Relaxation/drug effects ; Neurons/drug effects ; Time Factors
    • Abstract:
      Here we report on the action of the novel cyclo-depsipeptide anthelmintic, emodepside, on the body wall muscle of the parasitic nematode, Ascaris suum. Emodepside caused (i) muscle relaxation, (ii) inhibition of muscle contraction elicited by either acetylcholine (ACh), or the neuropeptide, AF2 (KHEYLRFamide) and (iii) a rapid relaxation of muscle tonically contracted by ACh. The inhibitory action of emodepside on the response to ACh was not observed in a denervated muscle strip, indicating that it may exert this action through the nerve cord, and not directly on the muscle. Electrophysiological recordings showed emodepside elicited a Ca(++)-dependent hyperpolarization of muscle cells. Furthermore, the response to emodepside was dependent on extracellular K+, similar to the action of the inhibitory neuropeptides PF1 and PF2 (SDPNFLRFamide and SADPNFLRFamide). Thus emodepside may act at the neuromuscular junction to stimulate release of an inhibitory neurotransmitter or neuromodulator, with a similar action to the PF1/PF2 neuropeptides.
    • Accession Number:
      0 (Anthelmintics)
      0 (Depsipeptides)
      0 (Peptides, Cyclic)
      054NR2135Y (Furylfuramide)
      N9YNS0M02X (Acetylcholine)
      SY7Q814VUP (Calcium)
      YZ647Y5GC9 (emodepside)
    • Publication Date:
      Date Created: 20030305 Date Completed: 20030611 Latest Revision: 20190818
    • Publication Date:
      20231215
    • Accession Number:
      10.1017/s0031182002002639
    • Accession Number:
      12613766