Target sites of anthelmintics.
This paper reviews sites of action of anthelmintic drugs including: (1) levamisole and pyrantel, which act as agonists at nicotinic acetylcholine receptors of nematodes; (2) the avermectins, which potentiate or gate the opening of glutamategated chloride channels found only in invertebrates; (3) piperazine, which acts as an agonist at GABA gated chloride channels on nematode muscle; (4) praziquantel, which increases the permeability of trematode tegument to calcium and results in contraction of the parasite muscle; (5) the benzimidazoles, like thiabendazole, which bind selectively to parasite beta-tubulin and prevents microtubule formation; (6) the proton ionophores, like closantel, which uncouple oxidative phosphorylation; (7) diamphenethide and clorsulon, which selectively inhibit glucose metabolism of Fasciola and; (8) diethylcarbamazine, which appears to interfere with arachidonic acid metabolism of filarial parasites and host. The review concludes with brief comments on the development of anthelmintics in the future.
Martin
R J
RJ
Department of Preclinical Veterinary Sciences, University of Edinburgh, Summerhall.
Robertson
A P
AP
Bjorn
H
H
D000595:Amino Acid Sequence; D000818:Animals; D000871:Anthelmintics / Q000494:pharmacology*; D001095:Arachidonic Acids / Q000378:metabolism; D005947:Glucose / Q000378:metabolism; D007473:Ion Channels / Q000037:antagonists & inhibitors; D008870:Microtubules / Q000187:drug effects; D008969:Molecular Sequence Data; D018733:Nicotinic Antagonists / Q000494:pharmacology; D010085:Oxidative Phosphorylation / Q000187:drug effects; D010539:Permeability / Q000187:drug effects; D011978:Receptors, Nicotinic / Q000737:chemistry
D000871:Anthelmintics; D001095:Arachidonic Acids; D007473:Ion Channels; D018733:Nicotinic Antagonists; D011978:Receptors, Nicotinic; D005947:Glucose