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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
1997-1-13
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pubmed:abstractText |
1. A cloned cDNA encoding a human 5-hydroxytryptamine3 receptor type A subunit (h5-HT3R-As) was transfected into human embryonic kidney (HEK 293) cells maintained in cell culture and a stable cell line expressing a high density of the recombinant receptor was selected. 2. Membrane homogenates prepared from transfected, but not untransfected, cells exhibited a homogeneous and saturable population (Bmax = 4.49 +/- 0.46 pmol mg-1 protein) of sites that bound the radiolabelled 5-HT3 receptor antagonist, [3H]-granisetron with high affinity (pKD = 8.87 +/- 0.08). Kinetic studies (at 37 degrees C) revealed rapid association (kappa +1 4.76 +/- 0.3 x 10(8) M-1 min-1) and dissociation (kappa -1 = 0.21 +/- 0.003 min-1) of the radioligand. 3. Selective and non-selective 5-HT3 receptor ligands competed for [3H]-granisetron binding with a rank order of potency (granisetron > ondansetron > meta-chlorophenylbiguanide > 5-HT > 2-methyl-5-HT > metoclopramide > > phenylbiguanide > cocaine > (+)-tubocurarine) identical to that established for 5-HT3 receptors endogenous to the human CNS. 4. In electrophysiological recordings performed on transfected cells, voltage-clamped at a holding potential of -60 mV, locally applied 5-HT (10 microM) evoked transient inward current responses that reversed in sign at a potential of -1.0 +/- 1.1 mV. Such responses were antagonized in a reversible manner by granisetron (1 nM). 5. The construction of a stable cell line expressing a high density of recombinant human 5-HT3 receptors which display appropriate pharmacology and function will assist in the further characterization of this receptor subtype and the exploration of species differences in 5-HT3 receptor pharmacology.
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-1364827,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-1407396,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-1413088,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-14907713,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-1533419,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-1715528,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-1718042,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-1797317,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-2076479,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-2402301,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-2472553,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-2543418,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-2809591,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-3000889,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-3839291,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-4202581,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-518835,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-6312838,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-6472484,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-6853562,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7509203,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7537814,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7539990,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7541281,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7565620,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7620711,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7683998,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7773546,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7790853,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7938165,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7969053,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7984267,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-7984286,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-8152523,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-8229003,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-8232790,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-8247158,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-841862,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-8419547,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-8436978,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-8528560,
http://linkedlifedata.com/resource/pubmed/commentcorrection/8818349-8848005
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
0007-1188
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
118
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1237-45
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pubmed:dateRevised |
2009-11-18
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pubmed:meshHeading |
pubmed-meshheading:8818349-Binding, Competitive,
pubmed-meshheading:8818349-Cells, Cultured,
pubmed-meshheading:8818349-Electrophysiology,
pubmed-meshheading:8818349-Granisetron,
pubmed-meshheading:8818349-Humans,
pubmed-meshheading:8818349-Kinetics,
pubmed-meshheading:8818349-Membrane Potentials,
pubmed-meshheading:8818349-Nicotinic Antagonists,
pubmed-meshheading:8818349-Receptors, Serotonin,
pubmed-meshheading:8818349-Serotonin Antagonists,
pubmed-meshheading:8818349-Tubocurarine
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pubmed:year |
1996
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pubmed:articleTitle |
Characterization of a human 5-hydroxytryptamine3 receptor type A (h5-HT3R-AS) subunit stably expressed in HEK 293 cells.
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pubmed:affiliation |
Department of Pharmacology and Clinical Pharmacology, Ninewells Hospital and Medical School, Dundee University, U.K.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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