Adipiplon Explained

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

Notes and References

  1. http://www.neurogen.com/products/gaba%20insomnia.html Pipeline Summary GABA: Adipiplon
  2. https://www.drugs.com/clinical_trials/neurogen-announces-adipiplon-preclinical-clinical-data-presented-neuroscience-2007-2614.html Neurogen Announces Adipiplon Preclinical and Clinical Data
  3. http://www.sleepreviewmag.com/sleep_report/2007-09-12_07.asp Meet Adipiplon: The New Insomnia Drug
  4. http://www.fiercebiotech.com/biotech/neurogen-announces-suspension-of-insomnia-study-adipiplon Neurogen Announces Suspension of Insomnia Study with Adipiplon