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Not to be confused with adipiodone.

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.[1]

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.[2][3][4] These trials were suspended after significant next-day side effects were discovered.[5]

See also

References

  1. ^ Vinkers CH, Olivier B, Hanania T, Min W, Schreiber R, Hopkins SC, et al. (October 2011). “Discriminative stimulus properties of GABAA receptor positive allosteric modulators TPA023, ocinaplon and NG2-73 in rats trained to discriminate chlordiazepoxide or zolpidem”. European Journal of Pharmacology. 668 (1–2): 190–193. doi:10.1016/j.ejphar.2011.06.054. PMID 21762686.
  2. ^ “Pipeline Summary GABA: Adipiplon”. Neurogen. Archived from the original on April 11, 2008.
  3. ^ “Neurogen Announces Adipiplon Preclinical and Clinical Data”.
  4. ^ “Meet Adipiplon: The New Insomnia Drug”. Sleep Review. Archived from the original on April 15, 2008.
  5. ^ “Neurogen Announces Suspension of Insomnia Study with Adipiplon”. Fierce Biotech. 14 July 2008.