
CAS
720690-73-3
Formulation
A solid
Purity
≥98%
MW
351,4
Shipment
-20
Long Term Storage
-20
Shelf Life
1460
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).{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}
ESCLUSIVAMENTE PER USO DI RICERCA (RUO) e non per uso terapeutico o diagnostico su uomini o animali. Il prodotto NON è un Dispositivo Medico o un Diagnostico in Vitro.
PRODUCT FOR RESEARCH USE ONLY (RUO) and not for therapeutic or diagnostic use on humans or animals. The product is NOT a Medical Device or an In-Vitro Diagnostic (IVD).