Antihistamine-1

Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

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

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

Research Areas >> Neurological Disease

CYP2D6:5.4 μM (IC50)

Antihistamine-1 (Compound 2) is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively[1].

[1]. Lavrador-Erb K, et al. The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia. Bioorg Med Chem Lett. 2010 May 1;20(9):2916-9.

Nigericin sodium salt | Talarozole | Senicapoc | Apigenin | E-4031 | 4-AMINOPYRIDINE | Cobicistat (GS-9350) | Loratadine | Ginsenoside Rg3 | TRAM-34 | Dofetilide | Ginsenoside Compound K | PAP-1 | Gemfibrozil | Histamine