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The development of a serotonin 5-HT2C receptor-binding assay using the LEADseeker Multimodality Imaging System

Key words: serotonin • GPCR receptor binding assay LEADseeker SPA Imaging Beads


In mammals, serotonin (5-hydroxytryptamine, 5-HT) is a regulator of neural transmission which induces its biological effect by binding to serotonin receptors.

The serotonin 5-HT2C receptor is a subtype of the serotonin receptor that belongs to the rhodopsin-like seven transmembrane superfamily of G protein-coupled receptors (1). 5-HT2C receptors are widely expressed in the brain and spinal cord and are particularly enriched in the choroid plexus (2). They are reported to play a significant role in disorders such as obesity (3, 4) and hyperactivity (4). It has also been demonstrated that the 5-HT2C receptors bind a wide range of drugs used in the treatment of psychiatric disorders such as depression and schizophrenia (5, 6).

This application note describes a 384-well serotonin 5-HT2C receptor-binding assay which has been developed using the LEADseeker™ Multimodality Imaging System.


Materials
Products used

LEADseeker Multimodality Imaging System 18-1140-71

Wheat Germ Agglutinin (WGA) PEI Type RPNQ0287
A PS SPA Imaging Beads

[N6-methyl-3H]Mesulergine TRK845


Other material required
Human recombinant 5-HT2C (Euroscreen ES-315-M)
edited form, receptor membrane preparation

Mianserin hydrochloride (Sigma M2525)

Ketanserin tartrate
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