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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2-3
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pubmed:dateCreated |
1997-4-3
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pubmed:abstractText |
Iloperidone (HP 873; 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy] -3- methoxyphenyl]ethanone) is a compound currently in clinical trials for the treatment of schizophrenia. Iloperidone displays affinity for dopamine D2 receptors and for 5-HT2A receptors and has a variety of in vivo activities suggestive of an atypical antipsychotic. Here we present an examination of the affinity of iloperidone to a variety of human and rat homologs of dopamine and 5-HT receptor subtypes. We employed receptor binding assays using membranes from cells stably expressing human dopamine D1, D2S, D2L, D3, D4 and D5 and 5-HT2A and 5-HT2C receptors and rat 5-HT6 and 5-HT7 receptors. Iloperidone displayed higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). Iloperidone displayed high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 and 21.6 nM, respectively), and was found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM). The potential implications of this receptor binding profile are discussed in comparison with data for other antipsychotic compounds.
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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/Antipsychotic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/DRD3 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/DRD4 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/DRD5 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Drd3 protein, rat,
http://linkedlifedata.com/resource/pubmed/chemical/Drd4 protein, rat,
http://linkedlifedata.com/resource/pubmed/chemical/Drd5 protein, rat,
http://linkedlifedata.com/resource/pubmed/chemical/Isoxazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine D1,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine D2,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine D3,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine D4,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine D5,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/iloperidone
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pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
0014-2999
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
19
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pubmed:volume |
317
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
417-23
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pubmed:dateRevised |
2005-11-17
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pubmed:meshHeading |
pubmed-meshheading:8997630-Animals,
pubmed-meshheading:8997630-Antipsychotic Agents,
pubmed-meshheading:8997630-Basal Ganglia Diseases,
pubmed-meshheading:8997630-CHO Cells,
pubmed-meshheading:8997630-Cricetinae,
pubmed-meshheading:8997630-Humans,
pubmed-meshheading:8997630-Isoxazoles,
pubmed-meshheading:8997630-Kinetics,
pubmed-meshheading:8997630-Piperidines,
pubmed-meshheading:8997630-Rats,
pubmed-meshheading:8997630-Receptors, Dopamine,
pubmed-meshheading:8997630-Receptors, Dopamine D1,
pubmed-meshheading:8997630-Receptors, Dopamine D2,
pubmed-meshheading:8997630-Receptors, Dopamine D3,
pubmed-meshheading:8997630-Receptors, Dopamine D4,
pubmed-meshheading:8997630-Receptors, Dopamine D5,
pubmed-meshheading:8997630-Receptors, Serotonin
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pubmed:year |
1996
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pubmed:articleTitle |
Iloperidone binding to human and rat dopamine and 5-HT receptors.
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pubmed:affiliation |
Neuroscience Research, Hoechst Marion Roussel, Inc., Bridgewater, NJ 08807-0800, USA. KONGSAM1@brwhcc3.hcc.com
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pubmed:publicationType |
Journal Article
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