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Development of an adrenergic α2a receptor binding assay using the LEADseeker Multimodality Imaging System

Key words: α2c receptor • GPCR • receptor binding assay • LEADseeker • SPA Imaging Beads


The α2-adrenergic receptors are G protein-coupled receptors that play a key role in the control of numerous physiological functions such as renal Na+ re-absorption, insulin secretion, platelet aggregation, and neurotransmitter release at sympathetic nerve endings (1). They consist of three highly homologous subtypes encoded by distinct genes: α2a, α2b, and α2c. Both α2a and α2c subtypes are required for normal presynaptic control of neurotransmitter release from sympathetic nerves from the heart and from central noradrenergic neurons. α2a adrenergic receptors inhibit transmitter release at high stimulation frequencies whilst the α2c subtype modulates neurotransmission at lower levels of nerve activity (2). The α2c receptor is distinguishable from α2a and α2b receptors by its sensitivity to prazosin (3).

This application note describes a 384-well adrenergic α2c receptor binding assay developed using the LEADseeker™ Multimodality Imaging System.


Materials
Products used
LEADseeker Multimodality Imaging System 18-1140-71

Wheat Germ Agglutinin (WGA) YOx RPNQ0270
SPA Imaging Beads

[0-methyl-3H]Rauwolscine TRK685


Other materials required
Human recombinant adrenergic α2c receptor membrane preparation (Euroscr
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