Interaction between enantiomers of mianserin and ORG3770 at 5-HT3 receptors in cultured mouse neuroblastoma cells
作者： A.R. Kooyman , R. Zwart , P.M.L. Vanderheijden , J.A. Van Hooft , H.P.M. Vijverberg
DOI: 10.1016/0028-3908(94)90081-7
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摘要: Abstract Stereoselective effects of mianserin and ORG3770 on serotonin 5-HT3 receptors in mouse neuroblastoma N1E-115 cells have been investigated radioligand binding whole-cell voltage clamp experiments. The specific [3H]GR65630 to recognition sites cell homogenates is reduced by their enantiomers. p Ki values the more potent (R)enantiomers are 8.44 8.62, respectively. 15 37 times than respective(S)enantiomers. racemates only 1.9 3.3 less corresponding (R)enantiomers. In experiments block 5-hydroxytryptamine(5-HT)-induced ion current with pIC50 8.52 for (R)mianserin 8.26 (R)enantiomer ORG3770. 24 145 blocking 5-HT-induced respective (S)enantiomers. 6 13 addition, partially reversed a low concentration its (S)enantiomer. results indicate that two enantiomers receptor-mediated mutually dependent manner.
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