rdf:type |
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lifeskim:mentions |
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pubmed:dateCreated |
1998-5-21
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pubmed:abstractText |
1. A human recombinant homo-oligomeric 5-HT3 receptor (h5-HT3A) expressed in a human embryonic kidney cell line (HEK 293) was characterized using the whole-cell recording configuration of the patch clamp technique. 2. 5-HT evoked transient inward currents (EC50 = 3.4 microM; Hill coefficient = 1.8) that were blocked by the 5-HT3 receptor antagonist ondansetron (IC50 = 103 pM) and by the non-selective agents metoclopramide (IC50 = 69 nM), cocaine (IC50 = 459 nM) and (+)-tubocurarine (IC50 = 2.8 microM). 3. 5-HT-induced currents rectified inwardly and reversed in sign (E5-HT) at a potential of -2.2 mV. N-Methyl-D-glucamine was finitely permeant. Permeability ratios PNa/PCs and PNMDG/PCs were 0.90 and 0.083, respectively. 4. Permeability towards divalent cations was assessed from measurements of E5-HT in media where Ca2+ and Mg2+ replaced Na+. PCa/PCs and PMg/PCs were calculated to be 1.00 and 0.61, respectively. 5. Single channel chord conductance (gamma) estimated from fluctuation analysis of macroscopic currents increased with membrane hyperpolarization from 243 fS at -40 mV to 742 fS at -100 mV. 6. Reducing [Ca2+]o from 2 to 0.1 mM caused an increase in the whole-cell current evoked by 5-HT. A concomitant reduction in [Mg2+]o produced further potentiation. Fluctuation analysis indicates that a voltage-independent augmentation of gamma contributes to this phenomenon. 7. The data indicate that homo-oligomeric receptors composed of h5-HT3A subunits form inwardly rectifying cation-selective ion channels of low conductance that are permeable to Ca2+ and Mg2+.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-1375636,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-1707717,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-1717313,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-1718042,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-2170596,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-2286832,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-2421791,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-2459620,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-2463926,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-2472553,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-2600815,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-2720311,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-312319,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-6296371,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7509203,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7520482,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7524560,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7537814,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7565620,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7566492,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7620711,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7683998,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7694755,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7778876,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7808432,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-7938165,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-8083751,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-8152523,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-8247158,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-8581403,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-8764583,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-8818349,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-8848005,
http://linkedlifedata.com/resource/pubmed/commentcorrection/9508827-9225291
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Calcium,
http://linkedlifedata.com/resource/pubmed/chemical/Cations, Divalent,
http://linkedlifedata.com/resource/pubmed/chemical/Cocaine,
http://linkedlifedata.com/resource/pubmed/chemical/Magnesium,
http://linkedlifedata.com/resource/pubmed/chemical/Meglumine,
http://linkedlifedata.com/resource/pubmed/chemical/Metoclopramide,
http://linkedlifedata.com/resource/pubmed/chemical/Ondansetron,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin, 5-HT3,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Sodium,
http://linkedlifedata.com/resource/pubmed/chemical/Tubocurarine
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pubmed:status |
MEDLINE
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pubmed:month |
Mar
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pubmed:issn |
0022-3751
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
507 ( Pt 3)
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
653-65
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pubmed:dateRevised |
2010-8-25
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pubmed:meshHeading |
pubmed-meshheading:9508827-Calcium,
pubmed-meshheading:9508827-Cations, Divalent,
pubmed-meshheading:9508827-Cell Line,
pubmed-meshheading:9508827-Cell Membrane Permeability,
pubmed-meshheading:9508827-Cocaine,
pubmed-meshheading:9508827-Electric Conductivity,
pubmed-meshheading:9508827-Evoked Potentials,
pubmed-meshheading:9508827-Humans,
pubmed-meshheading:9508827-Kinetics,
pubmed-meshheading:9508827-Magnesium,
pubmed-meshheading:9508827-Meglumine,
pubmed-meshheading:9508827-Metoclopramide,
pubmed-meshheading:9508827-Models, Chemical,
pubmed-meshheading:9508827-Ondansetron,
pubmed-meshheading:9508827-Receptors, Serotonin,
pubmed-meshheading:9508827-Receptors, Serotonin, 5-HT3,
pubmed-meshheading:9508827-Recombinant Proteins,
pubmed-meshheading:9508827-Serotonin,
pubmed-meshheading:9508827-Serotonin Antagonists,
pubmed-meshheading:9508827-Sodium,
pubmed-meshheading:9508827-Transfection,
pubmed-meshheading:9508827-Tubocurarine
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pubmed:year |
1998
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pubmed:articleTitle |
Ion permeation and conduction in a human recombinant 5-HT3 receptor subunit (h5-HT3A).
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pubmed:affiliation |
Department of Pharmacology and Neuroscience, Ninewells Hospital and Medical School, The University of Dundee, Dundee DD1 9SY, UK.
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pubmed:publicationType |
Journal Article
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