Formulation: A solid
Formal Name: 6-[(3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy]-N-methyl-3-pyridinecarboxamide
Purity: ≥98%
Formula Markup: C21H25N3O2
Formula Weight: 351,4
Shelf life (days): 1460
CAS Number: 720690-73-3
Notes: 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).{69016} 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).{69017}
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