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- W2048719783 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." @default.
- W2048719783 created "2016-06-24" @default.
- W2048719783 creator A5027453161 @default.
- W2048719783 creator A5045642237 @default.
- W2048719783 creator A5076963133 @default.
- W2048719783 date "2008-01-01" @default.
- W2048719783 modified "2023-09-29" @default.
- W2048719783 title "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" @default.
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- W2048719783 doi "https://doi.org/10.1016/j.ejphar.2007.09.020" @default.
- W2048719783 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2963108" @default.
- W2048719783 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17961544" @default.
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