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H4R antagonist 1

CAS No. : 1429375-54-1

產品活性：H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC₅₀ of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.

研究領域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶點：Histamine Receptor

In Vitro: The competitive binding assay against a wider panel of GPCR, ion channel, and transporters at the concentration of 10 μM reveals that H4R antagonist 1 (Compound 48) is highly selective for H4R. The inhibitory activity of H4R antagonist 1 against mouse H4R (IC₅₀=0.29 μM) is about 10 times weaker than that for human H4R.

In Vivo: H4R antagonist 1 (Compound 48) shows significant antipruritic and anti-inflammatory efficacy in Oxazolone-induced murine model mimicking human atopic dermatitis (AD).
In the [³⁵S]GTPγS functional assay, H4R antagonist 1 shows inhibitory activity against mouse H4R with an IC₅₀ of 0.69 μM.

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