GSK189254A

GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.

Product Specifications

CAS Number

[720690-73-3]

Product Name Alternative

GSK189254 (free base)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335, H412

Target

Histamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/GSK189254A.html

Purity

98.59

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C(NC)C(C=N1)=CC=C1OC2=CC(CC3)=C(C=C2)CCN3C4CCC4

Molecular Formula

C21H25N3O2

Molecular Weight

351.44

Precautions

H302, H315, H319, H335, H412

References & Citations

[1]Medhurst AD, et al. GSK189254, a novel H3 receptor antagonist that binds to histamine H3 receptors in Alzheimer's disease brain and improves cognitive performance in preclinical models. J Pharmacol Exp Ther. 2007 Jun;321 (3) :1032-45.|[2]Guo RX, et al. Differential effects of acute and repeat dosing with the H3 antagonist GSK189254 on the sleep-wake cycle and narcoleptic episodes in Ox-/- mice.Br J Pharmacol. 2009 May;157 (1) :104-17.