Adipiplon

Not to be confused with adipiodone.
Adipiplon
Clinical data
Routes of
administration		Oral
ATC code
  • none
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • 7-[(2-(3-fluoropyridin-2-yl)-1H-imidazol-1-yl)methyl]-2-methyl-8-propyl-[1,2,4]triazolo[1,5-c]pyrimidine
CAS Number
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H18FN7
Molar mass351.389 g·mol−1
3D model (JSmol)
  • n4c(C)nc1n4cnc(c1CCC)Cn2ccnc2-c3ncccc3F
  • InChI=1S/C18H18FN7/c1-3-5-13-15(22-11-26-17(13)23-12(2)24-26)10-25-9-8-21-18(25)16-14(19)6-4-7-20-16/h4,6-9,11H,3,5,10H2,1-2H3 checkY
  • Key:UAMAIHOEGLEXSV-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

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

Adipiplon is a subtype-selective GABAA receptor 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 can discriminate between α2 and α3, as well as showing a little affinity for the α1 or α5 subtypes — alpidem is selective for α3 over α2, but still has moderate affinity for α1, whereas adipiplon is highly α3-selective with little affinity for either α1, α2 or α5.

Adipiplon was being researched as a potential medication for the treatment of anxiety and insomnia, and in 2008 it was being used in Phase IIb trials.[1][2][3] These trials were suspended after significant next-day side effects were discovered.[4]

See also

[edit]

References

[edit]
  1. ^ Pipeline Summary GABA: Adipiplon Archived April 11, 2008, at the Wayback Machine
  2. ^ Neurogen Announces Adipiplon Preclinical and Clinical Data
  3. ^ Meet Adipiplon: The New Insomnia Drug Archived April 15, 2008, at the Wayback Machine
  4. ^ Neurogen Announces Suspension of Insomnia Study with Adipiplon



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