H4 Receptor antagonist 1

H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

H4 receptor:19 nM (IC50)

H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM[1].

H4 Receptor antagonist 1 indicates that metabolic stability in rat microsomes is very low with only 1% parent compound remaining after 10 min incubation[1].

[1]. Cramp S, et al. Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2516-9.

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