GSK189254

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). 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-Galphao cells expressing the human histamine H3 receptor (pA2 = 9.06). It inhibits increases in water intake induced by the histamine H3 receptor agonist R-(-)-alpha-methylhistamine (Cay-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).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: (Request formulation change), A solid. Solubility: DMSO: soluble with sonication/heat. lambdamax: 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.