dc.creator | Trailović, Saša | |
dc.creator | Marjanović, Đorđe | |
dc.creator | Tipton, James M. | |
dc.creator | Abongwa, Melanie | |
dc.creator | Zheng, Fudan | |
dc.creator | Choudhary, Shivani | |
dc.creator | Martin, Richard J. | |
dc.creator | Robertson, Alan P. | |
dc.date.accessioned | 2023-11-14T07:35:08Z | |
dc.date.available | 2023-11-14T07:35:08Z | |
dc.date.issued | 2016 | |
dc.identifier.uri | https://vet-erinar.vet.bg.ac.rs/handle/123456789/3346 | |
dc.description.abstract | Zolvix ® is a recently introduced anthelmintic drench containing monepantel as the active ingredient.
Monepantel has been demonstrated to act on deg-3/des-2 containing nAChRs in several nematodes as
a positive allosteric modulator. The drug produces hypercontraction of nematode muscle. We
investigated the effects of monepantel on muscle strips isolated form adult Ascaris suum. The drug did
not significantly increase baseline tension when applied on its own. Contractions induced by
acetylcholine and several cholininomimetic anthelmintics where antagonized by monepantel. Further
investigation revealed that the antagonism was non-competitive in nature. We also investigated the
effect of monepantel on nAChRs from O. dentatum heterologously expressed in Xenopus laevis
oocytes. We investigated the effects of monepantel on OD3, a levamisole preferring nAChR subtype,
OD4, a pyrantel preferring subtype and ACR-16 a nicotine preferring subtype. For each subtype tested
monepantel applied in isolation produced no measureable currents, nor did it produce currents in the
presence of choline. When monepantel was continuously applied it reduced the amplitude of
acetylcholine induced currents in a concentration dependent manner for the three nAChR subtypes
tested. In all three cases monepantel acted as a non-competitive antagonist on the expressed
receptors. ACR-16 was particularly sensitive to monepantel inhibition. Our findings suggest that the
mode of action of monepantel is more complex than previously described. | sr |
dc.language.iso | en | sr |
dc.publisher | Society of Toxicology | sr |
dc.relation | info:eu-repo/grantAgreement/MESTD/Technological Development (TD or TR)/31087/RS// | sr |
dc.relation | Research grants: NIH RO1 A1047194 to RJM & APR, Schlumberger Faculty for the Future Fellowship to MA & APR. JT Support: NIH T35 OD 012199-13 | sr |
dc.rights | restrictedAccess | sr |
dc.source | Antihelmintics : From discovery to resistance II, Captain’s Room: Marina Village Center: San Diego, CA- Feb. 9 - 12, 2016 | sr |
dc.subject | Zolvix | sr |
dc.subject | A.suum | sr |
dc.subject | O.dentatum | sr |
dc.subject | nAChR subtypes | sr |
dc.title | Effects of monepantel on nicotinic acetylcholine receptors from Ascaris suum and Oesophagostomum dentatum | sr |
dc.type | conferenceObject | sr |
dc.rights.license | ARR | sr |
dc.citation.spage | 11 | |
dc.citation.epage | 11 | |
dc.description.other | Book of Abstracts | sr |
dc.identifier.rcub | https://hdl.handle.net/21.15107/rcub_veterinar_3346 | |
dc.type.version | publishedVersion | sr |