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PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
1998-5-21
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+.
pubmed:grant
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
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
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
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
0022-3751
pubmed:author
pubmed:issnType
Print
pubmed:day
15
pubmed:volume
507 ( Pt 3)
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
653-65
pubmed:dateRevised
2010-8-25
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
pubmed:year
1998
pubmed:articleTitle
Ion permeation and conduction in a human recombinant 5-HT3 receptor subunit (h5-HT3A).
pubmed:affiliation
Department of Pharmacology and Neuroscience, Ninewells Hospital and Medical School, The University of Dundee, Dundee DD1 9SY, UK.
pubmed:publicationType
Journal Article
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