GSK-189,254

GSK-189,254
Identifiers

IUPAC name 6-[(3-cyclobutyl-1,2,4,5-tetrahydro-3-benzazepin-7-yl)oxy]-N-methylpyridine-3-carboxamide
CAS Number	720690-73-3^N
PubChem CID	9798547
ChemSpider	7974313^N
UNII	5T4TX6CO53
ChEMBL	CHEMBL517140^N
Chemical and physical data
Formula	C₂₁H₂₅N₃O₂
Molar mass	351.441 g/mol
3D model (JSmol)	Interactive image
SMILES c4cc1CCN(C3CCC3)CCc1cc4Oc(cc2)ncc2C(=O)NC
InChI 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)^N Key:WROHEWWOCPRMIA-UHFFFAOYSA-N^N
^NY (what is this?)

GSK-189,254 is a potent and selective H₃ histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H₃ receptor (K_i = 0.2nM) and selectivity of over 10,000x for H₃ over other histamine receptor subtypes. Animal studies have shown it to possess not only stimulant and nootropic effects, but also analgesic action suggesting a role for H₃ receptors in pain processing in the spinal cord. GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia, as well as possible use in the treatment of conditions such as narcolepsy, or neuropathic pain which do not respond well to conventional analgesic drugs.

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