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Drug ReportsGSK189254
GSK189254
Gsk189254 is a small molecule pharmaceutical. It is currently being investigated in clinical studies.
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Commercial
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Clinical
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Drug
General
Drug common nameGSK189254
INN
Description
GSK-189,254 is a potent and selective H3 histamine receptor inverse agonist developed by GlaxoSmithKline. It has subnanomolar affinity for the H3 receptor (Ki = 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.
Classification
Small molecule
Drug class
Image (chem structure or protein)Loading
Structure (InChI/SMILES or Protein Sequence)
CNC(=O)c1ccc(Oc2ccc3c(c2)CCN(C2CCC2)CC3)nc1
Identifiers
PDB
CAS-ID720690-73-3
RxCUI
ChEMBL IDCHEMBL517140
ChEBI ID
PubChem CID9798547
DrugBank
UNII ID
Target
No data
Variants
No data
Financial
No data
Trends
No data
Safety
Black-box Warning
No Black-box warning
Adverse Events
0 adverse events reported
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