Histamine receptor (H1R-H4R) is a subtype of G protein-coupled receptor that attracts histamine as the majority of its endogenous ligand. The receptors are extensively dispersed throughout the body and play a pivotal part in the occurrence of numerous allergy disorders. Noteworthy, histamine receptors have been targeted by drugs with anti-inflammatory, anti-ulcer, and sleep-inducing characteristics in the clinic. In the future, histamine receptors might be used as therapeutic targets for disorders such as schizophrenia. Therefore, advancing the development of a functional assay for histamine receptors has great meaning.
Fig.1 Histamine receptor expression on mast cells and their possible sensitivity to histamine.1
Creative Biolabs combines in vitro cell-based assay with histamine receptors functional assay and has successfully developed an efficient and robust Magic™ in vitro cell-based histamine receptor functional assay service. We measure second messenger accumulation and calcium flux in response to histamine receptor-ligand interactions, which is based on the fact that H2 receptors paired with Gs evoke cAMP accumulation, H3 and H4 receptors connected to Gi/o prevent cAMP accumulation, and H1 receptors coupled to Gq regulate Ca2+ mobilization.
Creative Biolabs consistently develops and innovates the technological platform in order to meet market demand, aiming to supply the most advanced technology and top-quality services to global customers. Accordingly, our Magic™ in vitro cell-based histamine receptor functional assay service will benefit global customers with:
Fig.2 The signaling pathway of histamine receptors.2
Representative Data
Data 1: This study evaluated intra-ER Ca2+ levels by producing a FRET-based ER Ca2+ sensor, D4ER, regulated by the mSncg promoter, in mouse retinal ganglion cells (RGCs) specifically, in order to definitely confirm the effective blockage of Ca2+ inflow by maprotiline, probably by suppression of histamine receptor H1-mediated Ca2+ release from the ER.
The findings revealed that optic nerve crush (ONC) drastically reduced ER Ca2+ concentrations in RGCs, but maprotiline maintained ER Ca2+ concentrations at considerably greater levels.
Fig.3 Ex vivo measurement of ER Ca2+.3
Data 2: Fluorescence studies of intracellular Ca2+ levels revealed that histamine triggered Ca2+ mobilization. The co-treatment of cells with histamine and the antihistamines DES or CIM resulted in a significant reduction. These findings support the concept that H1 and H2 are present in P19 neurons and play a role in histamine-induced Ca2+ mobilization. The addition of vDAO reduced the Ca2+ signal elicited by histamine, which should be related to the oxidative breakdown of histamine by this enzyme.
Fig.4 The impact of vDAO, histamine, and antihistamine medications on the intracellular calcium concentrations of P19 neurons.4
Creative Biolabs consistently develops and innovates the technological platform in order to meet market demand, aiming to supply the most advanced technology and top-quality services to global customers. If you're interested in learning more about our Magic™ in vitro cell-based histamine receptor functional assay service, please don't hesitate to contact us. Everyone here is excited to start working with you immediately.
References
For Research Use Only.
