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.

Product Specifications

CAS Number

[1186430-60-3]

UNSPSC

12352005

Target

Cytochrome P450; Histamine Receptor; Potassium Channel

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/Antihistamine-1.html

Purity

99.08

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC1=CN(C2CCN(C3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)N=C1

Molecular Formula

C23H24FN5

Molecular Weight

389.47

References & Citations

[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.