FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2892019072> ?p ?o ?g. }

• W2892019072 endingPage "1279" @default.
• W2892019072 startingPage "1270" @default.
• W2892019072 abstract "Nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels involved in neuromuscular transmission. In nematodes, muscle nAChRs are targets of antiparasitic drugs. Bephenium is an anthelmintic compound whose molecular action in the free-living nematode <i>Caenorhabditis elegans</i>, which is a model for anthelmintic drug discovery, is poorly known. We explored the effect of bephenium on <i>C. elegans</i> locomotion and applied single-channel recordings to identify its molecular target, mechanism of action, and selectivity between mammalian and <i>C. elegans</i> nAChRs. As in parasites, bephenium paralyzes <i>C. elegans</i>. A mutant strain lacking the muscle levamisole-sensitive nAChR (L-AChR) shows full resistance to bephenium, indicating that this receptor is the target site. Bephenium activates L-AChR channels from larvae muscle cells in the micromolar range. Channel activity is similar to that elicited by levamisole, appearing mainly as isolated brief openings. Our analysis revealed that bephenium is an agonist of L-AChR and an open-channel blocker at higher concentrations. It also activates mammalian muscle nAChRs. Opening events are significantly briefer than those elicited by ACh and do not appear in activation episodes at a range of concentrations, indicating that it is a very weak agonist of mammalian nAChRs. Recordings in the presence of ACh showed that bephenium acts as a voltage-dependent channel blocker and a low-affinity agonist. Molecular docking into homology-modeled binding-site interfaces represent the binding mode of bephenium that explains its partial agonism. Given the great diversity of helminth nAChRs and the overlap of their pharmacological profiles, unraveling the basis of drug receptor-selectivity will be required for rational design of anthelmintic drugs." @default.
• W2892019072 created "2018-09-27" @default.
• W2892019072 creator A5015191263 @default.
• W2892019072 creator A5032914418 @default.
• W2892019072 creator A5036636270 @default.
• W2892019072 creator A5047559151 @default.
• W2892019072 date "2018-09-06" @default.
• W2892019072 modified "2023-10-05" @default.
• W2892019072 title "Activation of<i>Caenorhabditis elegans</i>Levamisole-Sensitive and Mammalian Nicotinic Receptors by the Antiparasitic Bephenium" @default.
• W2892019072 cites W1483942114 @default.
• W2892019072 cites W1513183398 @default.
• W2892019072 cites W1538156864 @default.
• W2892019072 cites W1605667399 @default.
• W2892019072 cites W1954391111 @default.
• W2892019072 cites W1975972945 @default.
• W2892019072 cites W1978294750 @default.
• W2892019072 cites W1984662835 @default.
• W2892019072 cites W1987268954 @default.
• W2892019072 cites W1988602968 @default.
• W2892019072 cites W1997439841 @default.
• W2892019072 cites W1998604377 @default.
• W2892019072 cites W2003744323 @default.
• W2892019072 cites W2015202250 @default.
• W2892019072 cites W2020042478 @default.
• W2892019072 cites W2024471679 @default.
• W2892019072 cites W2042490928 @default.
• W2892019072 cites W2045066478 @default.
• W2892019072 cites W2050224291 @default.
• W2892019072 cites W2053821073 @default.
• W2892019072 cites W2055547557 @default.
• W2892019072 cites W2065122583 @default.
• W2892019072 cites W2066142272 @default.
• W2892019072 cites W2074005920 @default.
• W2892019072 cites W2081307064 @default.
• W2892019072 cites W2084167390 @default.
• W2892019072 cites W2087519842 @default.
• W2892019072 cites W2090690189 @default.
• W2892019072 cites W2095282287 @default.
• W2892019072 cites W2095784896 @default.
• W2892019072 cites W2099277573 @default.
• W2892019072 cites W2105668062 @default.
• W2892019072 cites W2111915171 @default.
• W2892019072 cites W2117515977 @default.
• W2892019072 cites W2119920331 @default.
• W2892019072 cites W2123668698 @default.
• W2892019072 cites W2128505545 @default.
• W2892019072 cites W2129455301 @default.
• W2892019072 cites W2131012228 @default.
• W2892019072 cites W2142837476 @default.
• W2892019072 cites W2143014450 @default.
• W2892019072 cites W2152806181 @default.
• W2892019072 cites W2169051367 @default.
• W2892019072 cites W2234292754 @default.
• W2892019072 cites W2317519491 @default.
• W2892019072 cites W2410867251 @default.
• W2892019072 cites W2466579682 @default.
• W2892019072 cites W2524130802 @default.
• W2892019072 cites W2594780853 @default.
• W2892019072 cites W2596453412 @default.
• W2892019072 cites W2612453616 @default.
• W2892019072 cites W2802093561 @default.
• W2892019072 cites W2804849250 @default.
• W2892019072 cites W4234444023 @default.
• W2892019072 cites W4237567990 @default.
• W2892019072 cites W4254946208 @default.
• W2892019072 doi "https://doi.org/10.1124/mol.118.113357" @default.
• W2892019072 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/30190363" @default.
• W2892019072 hasPublicationYear "2018" @default.
• W2892019072 type Work @default.
• W2892019072 sameAs 2892019072 @default.
• W2892019072 citedByCount "3" @default.
• W2892019072 countsByYear W28920190722022 @default.
• W2892019072 countsByYear W28920190722023 @default.
• W2892019072 crossrefType "journal-article" @default.
• W2892019072 hasAuthorship W2892019072A5015191263 @default.
• W2892019072 hasAuthorship W2892019072A5032914418 @default.
• W2892019072 hasAuthorship W2892019072A5036636270 @default.
• W2892019072 hasAuthorship W2892019072A5047559151 @default.
• W2892019072 hasBestOaLocation W28920190721 @default.
• W2892019072 hasConcept C104317684 @default.
• W2892019072 hasConcept C170493617 @default.
• W2892019072 hasConcept C185592680 @default.
• W2892019072 hasConcept C188987157 @default.
• W2892019072 hasConcept C18903297 @default.
• W2892019072 hasConcept C203014093 @default.
• W2892019072 hasConcept C2775910092 @default.
• W2892019072 hasConcept C2776908094 @default.
• W2892019072 hasConcept C2778938600 @default.
• W2892019072 hasConcept C2778944004 @default.
• W2892019072 hasConcept C2781325985 @default.
• W2892019072 hasConcept C50254741 @default.
• W2892019072 hasConcept C55493867 @default.
• W2892019072 hasConcept C58732023 @default.
• W2892019072 hasConcept C80161118 @default.
• W2892019072 hasConcept C82617044 @default.
• W2892019072 hasConcept C86803240 @default.
• W2892019072 hasConcept C95444343 @default.
• W2892019072 hasConcept C98274493 @default.

• next