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Development of a histamine H1 receptor binding assay using the LEADseeker Multimodality Imaging System

Key words: H1 receptor • GPCR • receptor binding assay • LEADseeker • SPA Imaging Beads


Histamine is a biogenic amine that plays important pathophysiological roles in central and peripheral tissues. Generally released from stimulated mast cells, it contributes to several biological processes that characterize allergic responses (1).The function of histamine is mediated via four G protein-coupled receptors, H1, H2, H3 and H4 (2). H1 receptor antagonists are one of the most commonly used class of drugs used to relieve the symptoms of allergic diseases, such as allergic rhinitis, atopic dermatitis, psoriasis and allergic conjunctivitis (3). The H1 receptor is thought to be involved in mediating inflammatory responses via effects on cytokine production (4).

This application note describes a 384-well histamine H1 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 SPA RPNQ0270
Imaging Beads

[pyridinyl-5-3H]Pyrilamine TRK608


Other materials required
Human recombinant Histamine (Euroscreen, ES-390-M)
H1 receptor membrane preparation

Pyrilamine maleate salt (Sigma, P5514)

Triprolidine hydrochloride (Sigma, T6764)
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