Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2-3
pubmed:dateCreated
2008-1-1
pubmed:abstractText
The ability of the sigma(1) receptor to interact with a huge range of drug structural classes coupled with its wide distribution in the body has contributed to it being implicated as a possible therapeutic target for a broad array of disorders ranging from substance abuse to depression to Alzheimer's disease. Surprisingly, the reported affinity values for some sigma(1) receptor ligands vary more than 50-fold. The potential of the sigma(1) receptor as a pharmacotherapeutic target prompted us to develop an unambiguous assay system for measuring the affinity of ligands to the cloned human sigma(1) receptor. In the course of characterizing this system and determining the true affinity values for almost three dozen compounds, it was discovered that some dopamine D(4) receptor selective compounds bind sigma(1) receptors with high affinity. A systematic analysis of haloperidol-like compounds revealed a clear structure-affinity relationship amongst clinically relevant butyrophenones. The antidepressant fluvoxamine, the drug of abuse methamphetamine, and the neurosteroid progesterone were amongst the many ligands whose interactions with the sigma(1) receptor were confirmed with our screening assay.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
http://linkedlifedata.com/resource/pubmed/chemical/Butyrophenones, http://linkedlifedata.com/resource/pubmed/chemical/Central Nervous System Agents, http://linkedlifedata.com/resource/pubmed/chemical/Dopamine Agents, http://linkedlifedata.com/resource/pubmed/chemical/Fluvoxamine, http://linkedlifedata.com/resource/pubmed/chemical/Haloperidol, http://linkedlifedata.com/resource/pubmed/chemical/Ligands, http://linkedlifedata.com/resource/pubmed/chemical/Methamphetamine, http://linkedlifedata.com/resource/pubmed/chemical/Pentazocine, http://linkedlifedata.com/resource/pubmed/chemical/Progesterone, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Dopamine D4, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, sigma, http://linkedlifedata.com/resource/pubmed/chemical/Tritium, http://linkedlifedata.com/resource/pubmed/chemical/sigma-1 receptor
pubmed:status
MEDLINE
pubmed:month
Jan
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
14
pubmed:volume
578
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
123-36
pubmed:dateRevised
2011-9-26
pubmed:meshHeading
pubmed-meshheading:17961544-Binding, Competitive, pubmed-meshheading:17961544-Butyrophenones, pubmed-meshheading:17961544-Cell Line, Tumor, pubmed-meshheading:17961544-Central Nervous System Agents, pubmed-meshheading:17961544-Cloning, Molecular, pubmed-meshheading:17961544-Dopamine Agents, pubmed-meshheading:17961544-Dose-Response Relationship, Drug, pubmed-meshheading:17961544-Fluvoxamine, pubmed-meshheading:17961544-Haloperidol, pubmed-meshheading:17961544-Humans, pubmed-meshheading:17961544-Ligands, pubmed-meshheading:17961544-Methamphetamine, pubmed-meshheading:17961544-Molecular Structure, pubmed-meshheading:17961544-Pentazocine, pubmed-meshheading:17961544-Progesterone, pubmed-meshheading:17961544-Protein Binding, pubmed-meshheading:17961544-Radioligand Assay, pubmed-meshheading:17961544-Receptors, Dopamine D4, pubmed-meshheading:17961544-Receptors, sigma, pubmed-meshheading:17961544-Reproducibility of Results, pubmed-meshheading:17961544-Structure-Activity Relationship, pubmed-meshheading:17961544-Transfection, pubmed-meshheading:17961544-Tritium
pubmed:year
2008
pubmed:articleTitle
An unambiguous assay for the cloned human sigma1 receptor reveals high affinity interactions with dopamine D4 receptor selective compounds and a distinct structure-affinity relationship for butyrophenones.
pubmed:affiliation
Department of Pharmacology & Neuroscience, University of North Texas Health Science Center, Fort Worth, TX 79107, USA.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't, Research Support, N.I.H., Extramural