GSK-189254

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.^[1] Animal studies have shown it to possess not only stimulant and nootropic effects,^[2] but also analgesic action suggesting a role for H₃ receptors in pain processing in the spinal cord.^[3] GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia,^[4] as well as possible use in the treatment of conditions such as narcolepsy,^[5] or neuropathic pain which do not respond well to conventional analgesic drugs.^[6]

CAS Number

• 720690-73-3 ^N

PubChem CID

• 9798547

ChemSpider

• 7974313 ^N

UNII

• 5T4TX6CO53

Quick facts Identifiers, CAS Number ...

GSK-189254

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
CompTox Dashboard (EPA)	DTXSID801005982
Chemical and physical data
Formula	C21H25N3O2
Molar mass	351.450 g·mol−1
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
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