Adipiplon

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Adipiplon
Systematic (IUPAC) name
7-[(2-(3-fluoropyridin-2-yl)-1H-imidazol-1-yl)methyl]-2-methyl-8-propyl-[1,2,4]triazolo[1,5-c]pyrimidine
Identifiers
CAS number 840486-93-3
ATC code  ?
PubChem  ?
Chemical data
Formula C18H18FN7 
Mol. mass 351.38 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status

Investigational New Drug

Routes  ?

Adipiplon (NG2-73) is an anxiolytic drug developed by Neurogen Corporation. It has similar effects to benzodiazepine drugs, but is structurally distinct and so is classed as a nonbenzodiazepine anxiolytic.

Adipiplon is a subtype selective GABAA partial agonist, which binds preferentially to the α3 subtype. This is significant as while several previous nonbenzodiazepine drugs have been developed that are selective for α2/3 over the other subtypes, adipiplon is one of the first drugs selected for clinical development which is able to discriminate between α2 and α3, as well as showing little affinity for the α1 or α5 subtypes - alpidem is selective for α3 over α2, but still has moderate affinity to α1, whereas adipiplon is highly α3-selective with little affinity for either α1, α2 or α5.

Adipiplon is being researched as a potential medication for the treatment of anxiety and insomnia, and is currently (as of 2008) in Phase IIb trials.[1][2][3]


[edit] References

  1. ^ Pipeline Summary GABA: Adipiplon
  2. ^ Neurogen Announces Adipiplon Preclinical and Clinical Data
  3. ^ Meet Adipiplon: The New Insomnia Drug