ArticleEuropean journal of pharmacology2008
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.
Article in European journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Novel dopamine 4 receptor ligands differentially ameliorate ADHD-like behaviors in spontaneously hypertensive rats.Psychopharmacology · 2026Article
- Article
- Synthesis and Pharmacological Characterization of a Difluorinated Analogue of Reduced Haloperidol as a Sigma-1 Receptor Ligand.ACS chemical neuroscience · 2023Article
- Pridopidine Promotes Synaptogenesis and Reduces Spatial Memory Deficits in the Alzheimer's Disease APP/PS1 Mouse Model.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2022Article
- Intracellular dynamics of the Sigma-1 receptor observed with super-resolution imaging microscopy.PloS one · 2022Article
- Underlying Susceptibility to Eating Disorders and Drug Abuse: Genetic and Pharmacological Aspects of Dopamine D4 Receptors.Nutrients · 2020Review
- Activation of the sigma-1 receptor by haloperidol metabolites facilitates brain-derived neurotrophic factor secretion from human astroglia.Neurochemistry international · 2017Article
- Sigma receptors [σRs]: biology in normal and diseased states.Journal of receptor and signal transduction research · 2016Article
- Substituted methcathinones differ in transporter and receptor interactions.Biochemical pharmacology · 2013Article
- A 96-well filtration method for radioligand binding analysis of σ receptor ligands.Journal of pharmaceutical and biomedical analysis · 2012Article
- Determination of a highly selective mixed-affinity sigma receptor ligand, in rat plasma by ultra performance liquid chromatography mass spectrometry and its application to a pharmacokinetic study.Journal of chromatography. B, Analytical technologies in the biomedical and life sciences · 2012Article
- Robotic large-scale application of wheat cell-free translation to structural studies including membrane proteins.New biotechnology · 2011Article
- Design, synthesis, radiolabeling, and in vivo evaluation of carbon-11 labeled N-[2-[4-(3-cyanopyridin-2-yl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a potential positron emission tomography tracer for the dopamine D(4) receptors.Journal of medicinal chemistry · 2010Article
- A prototypical Sigma-1 receptor antagonist protects against brain ischemia.Brain research · 2007Article
- Brain-derived neurotrophic factor for high-throughput evaluation of selective Sigma-1 receptor ligands.Journal of pharmacological and toxicological methodsArticle
- Identification of the Sigma-2 Receptor: Distinct from the Progesterone Receptor Membrane Component 1 (PGRMC1).Journal of alcoholism and drug dependenceArticle
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
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.
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