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- W1554828019 endingPage "965" @default.
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- W1554828019 abstract "Background and Purpose The activation of α9α10 nicotinic cholinergic receptors ( nAChRs ) present at the synapse between efferent olivocochlear fibres and cochlear hair cells can prevent acoustic trauma. Hence, pharmacological potentiators of these receptors could be useful therapeutically. In this work, we characterize ascorbic acid as a positive modulator of recombinant α9α10 nAChRs . Experimental Approach ACh ‐evoked responses were analysed under two‐electrode voltage‐clamp recordings in X enopus laevis oocytes injected with α9 and α10 cRNAs . Key Results Ascorbic acid potentiated ACh responses in X . laevis oocytes expressing α9α10 (but not α4β2 or α7) nAChRs , in a concentration‐dependent manner, with an effective concentration range of 1–30 mM . The compound did not affect the receptor's current–voltage profile nor its apparent affinity for ACh , but it significantly enhanced the maximal evoked currents (percentage of ACh maximal response, 240 ± 20%). This effect was specific for the L form of reduced ascorbic acid. Substitution of the extracellular cysteine residues present in loop C of the ACh binding site did not affect the potentiation. Ascorbic acid turned into a partial agonist of α9α10 nAChRs bearing a point mutation at the pore domain of the channel ( TM2 V13′T mutant). A positive allosteric mechanism of action rather than an antioxidant effect of ascorbic acid is proposed. Conclusions and Implications The present work describes one of the few agents that activates or potentiates α9α10 nAChRs and leads to new avenues for designing drugs with potential therapeutic use in inner ear disorders." @default.
- W1554828019 created "2016-06-24" @default.
- W1554828019 creator A5024223170 @default.
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- W1554828019 creator A5043076508 @default.
- W1554828019 creator A5068838016 @default.
- W1554828019 creator A5091877247 @default.
- W1554828019 date "2013-01-24" @default.
- W1554828019 modified "2023-10-17" @default.
- W1554828019 title "Positive modulation of the α9α10 nicotinic cholinergic receptor by ascorbic acid" @default.
- W1554828019 cites W1497840173 @default.
- W1554828019 cites W1513702727 @default.
- W1554828019 cites W1570379376 @default.
- W1554828019 cites W1916800927 @default.
- W1554828019 cites W1964744325 @default.
- W1554828019 cites W1965278459 @default.
- W1554828019 cites W1966918903 @default.
- W1554828019 cites W1969549620 @default.
- W1554828019 cites W1969873523 @default.
- W1554828019 cites W1973602321 @default.
- W1554828019 cites W1978686647 @default.
- W1554828019 cites W1979158135 @default.
- W1554828019 cites W1980607589 @default.
- W1554828019 cites W1982626792 @default.
- W1554828019 cites W1986519531 @default.
- W1554828019 cites W1987204625 @default.
- W1554828019 cites W1987322407 @default.
- W1554828019 cites W1987370192 @default.
- W1554828019 cites W1992191480 @default.
- W1554828019 cites W1993926377 @default.
- W1554828019 cites W1994208375 @default.
- W1554828019 cites W1994980249 @default.
- W1554828019 cites W1995002017 @default.
- W1554828019 cites W1996673658 @default.
- W1554828019 cites W1997241346 @default.
- W1554828019 cites W1998093640 @default.
- W1554828019 cites W2000449705 @default.
- W1554828019 cites W2003867505 @default.
- W1554828019 cites W2012482374 @default.
- W1554828019 cites W2020372897 @default.
- W1554828019 cites W2020708235 @default.
- W1554828019 cites W2023651885 @default.
- W1554828019 cites W2024573050 @default.
- W1554828019 cites W2030969645 @default.
- W1554828019 cites W2036563492 @default.
- W1554828019 cites W2038111220 @default.
- W1554828019 cites W2039109065 @default.
- W1554828019 cites W2039221969 @default.
- W1554828019 cites W2039583391 @default.
- W1554828019 cites W2040621315 @default.
- W1554828019 cites W2044595919 @default.
- W1554828019 cites W2047687145 @default.
- W1554828019 cites W2048509522 @default.
- W1554828019 cites W2052658348 @default.
- W1554828019 cites W2056351808 @default.
- W1554828019 cites W2056488583 @default.
- W1554828019 cites W2059454447 @default.
- W1554828019 cites W2065283382 @default.
- W1554828019 cites W2065935683 @default.
- W1554828019 cites W2069380892 @default.
- W1554828019 cites W2074428623 @default.
- W1554828019 cites W2075820232 @default.
- W1554828019 cites W2077283202 @default.
- W1554828019 cites W2077904047 @default.
- W1554828019 cites W2094426376 @default.
- W1554828019 cites W2103001459 @default.
- W1554828019 cites W2103933289 @default.
- W1554828019 cites W2108956277 @default.
- W1554828019 cites W2112693462 @default.
- W1554828019 cites W2115827933 @default.
- W1554828019 cites W2133675069 @default.
- W1554828019 cites W2138961317 @default.
- W1554828019 cites W2141102948 @default.
- W1554828019 cites W2147285542 @default.
- W1554828019 cites W2147734514 @default.
- W1554828019 cites W2155687897 @default.
- W1554828019 cites W2156983843 @default.
- W1554828019 cites W2158266563 @default.
- W1554828019 cites W2239664554 @default.
- W1554828019 cites W2403261315 @default.
- W1554828019 cites W4251365796 @default.
- W1554828019 cites W4327635065 @default.
- W1554828019 doi "https://doi.org/10.1111/j.1476-5381.2012.02221.x" @default.
- W1554828019 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3631383" @default.
- W1554828019 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/22994414" @default.
- W1554828019 hasPublicationYear "2013" @default.
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