1186430-60-3

1186430-60-3 structure

Name: Antihistamine-1
Chemical Name: Antihistamine-1
CAS Number: 1186430-60-3
Molecular Formula: C₂₃H₂₄FN₅
Molecular Weight: 389.47
Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
Create Date: 2018-04-09 18:36:35
Modify Date: 2025-08-25 12:56:00
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.

Name	Antihistamine-1

Description	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.
Related Catalog	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
Target	CYP2D6:5.4 μM (IC50)
In Vitro	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].
References	[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.