A histamine H3 receptor antagonist
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GSK189254

Item No. 36705

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide
CAS Number
720690-73-3
Synonyms
  • GSK189254A
Molecular Formula
C21H25N3O2
Formula Weight
351.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble with sonication/heat
λmax
239 nm
SMILES
O=C(C1=CC=C(OC2=CC=C3C(CCN(C4CCC4)CC3)=C2)N=C1)NC
InChi Code
InChI=1S/C21H25N3O2/c1-22-21(25)17-6-8-20(23-14-17)26-19-7-5-15-9-11-24(18-3-2-4-18)12-10-16(15)13-19/h5-8,13-14,18H,2-4,9-12H2,1H3,(H,22,25)
InChi Key
WROHEWWOCPRMIA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $121

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    10 mg

    $217

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    25 mg

    $421

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    Product Description

    GSK189254 is a histamine H3 receptor antagonist (Kis = 0.13, 0.68, and 1.74 nM for the recombinant human, rat, and mouse receptors, respectively).1 It is selective for the histamine H3 receptor over a panel of 50 receptors and ion channels at 1 µM. GSK189254 prevents imetit-induced decreases in forskolin-stimulated cAMP accumulation in HEK293-Gαo cells expressing the human histamine H3 receptor (pA2 = 9.06). It inhibits increases in water intake induced by the histamine H3 receptor agonist R-(–)-α-methylhistamine (Item No. 25601) and reverses scopolamine-induced memory deficits in the passive avoidance test in rats. GSK189254 increases hindlimb grip force in a rat model of monoiodoacetate-induced osteoarthritic pain and increases the paw withdrawal threshold in a rat model of spinal nerve ligation-induced neuropathic pain (ED50s = 0.77 and 1.5 mg/kg, i.p., respectively).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Medhurst, A.D., Atkins, A.R., Beresford, I.J., 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. 321(3), 1032-1045 (2007).

    2. Hsieh, G.C., Honore, P., Pai, M., et al. Antinociceptive effects of histamine H3 receptor antagonist in the preclinical models of pain in rats and the involvement of central noradrenergic systems. Brain Res. 1354, 74-84 (2010).