rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1-3
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pubmed:dateCreated |
1997-5-6
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pubmed:abstractText |
5-HT3 receptor-mediated ion currents evoked by the full agonists 5-hydroxy-tryptamine (5-HT), quaternary 5-HT (5-HTQ), meta-chlorophenylbiguanide (mCPBG) and the partial agonists dopamine and tryptamine have been investigated in whole-cell voltage clamp experiments on N1E-115 mouse neuroblastoma cells. All agonists desensitize the 5-HT3 receptor completely with a steep concentration dependence and a potency order of: mCPBG > 5-HTQ approximately 5-HT > > tryptamine > dopamine. The time course of recovery from desensitization depends on the agonist used. Recovery from partial agonist-induced desensitization is single exponential, whereas the desensitization induced by full agonists recovers with sigmoid kinetics, suggesting at least 3 transitions between 4 states. It is concluded that full and partial agonists induce distinct desensitized states.
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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/1-(3-chlorophenyl)biguanide,
http://linkedlifedata.com/resource/pubmed/chemical/Biguanides,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin, 5-HT3,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Receptor Agonists,
http://linkedlifedata.com/resource/pubmed/chemical/Tetraethylammonium,
http://linkedlifedata.com/resource/pubmed/chemical/Tetraethylammonium Compounds
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pubmed:status |
MEDLINE
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pubmed:issn |
1079-9893
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
267-77
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:9029495-Animals,
pubmed-meshheading:9029495-Biguanides,
pubmed-meshheading:9029495-Evoked Potentials,
pubmed-meshheading:9029495-Mice,
pubmed-meshheading:9029495-Receptors, Serotonin,
pubmed-meshheading:9029495-Receptors, Serotonin, 5-HT3,
pubmed-meshheading:9029495-Serotonin,
pubmed-meshheading:9029495-Serotonin Receptor Agonists,
pubmed-meshheading:9029495-Tetraethylammonium,
pubmed-meshheading:9029495-Tetraethylammonium Compounds,
pubmed-meshheading:9029495-Tumor Cells, Cultured
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pubmed:articleTitle |
Full and partial agonists induce distinct desensitized states of the 5-HT3 receptor.
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pubmed:affiliation |
Research Institute of Toxicology, Utrecht University, The Netherlands.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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