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Sigma Receptor Binding Assays

Authors :
Uyen B. Chu
Arnold E. Ruoho
Source :
Current Protocols in Pharmacology
Publication Year :
2015
Publisher :
Wiley, 2015.

Abstract

Sigma receptors, both Sigma-1(S1R) and Sigma-2 (S2R), are small molecule-regulated, primarily endoplasmic reticulum (ER) membrane-associated sites. A number of drugs bind to sigma receptors, including the antipsychotic haloperidol and (+)-pentazocine, an opioid analgesic. Sigma receptors are implicated in many central nervous system disorders, in particular Alzheimer's disease and conditions associated with motor control, such as Amyotrophic Lateral Sclerosis (ALS). Described in this unit are radioligand binding assays used for the pharmacological characterization of S1R and S2R. Methods detailed include a radioligand saturation binding assay for defining receptor densities and a competitive inhibition binding assay employing [³H]-(+)-pentazocine for identifying and characterizing novel ligands that interact with S1R. Procedures using [³H]-1,3-di(2-tolyl)guanidine ([³H]-DTG), a nonselective sigma receptor ligand, are described for conducting a saturation binding and competitive inhibition assays for the S2R site. These protocols are of value in drug discovery in identifying new sigma ligands and in the characterization of these receptors.

Details

ISSN :
19348290 and 19348282
Volume :
71
Database :
OpenAIRE
Journal :
Current Protocols in Pharmacology
Accession number :
edsair.doi.dedup.....abcc704bba7fea56dfc4b96b236b1a6f
Full Text :
https://doi.org/10.1002/0471141755.ph0134s71