Indiplon is a nonbenzodiazepine, hypnotic sedative. Indiplon works by enhancing the action of the inhibitory neurotransmitter GABA, like most other nonbenzodiazepine sedatives. It primarily binds to the α1 subunits of the GABAA receptors in the brain. Indiplon was approved for the treatment of insomnia. Like other non-benzodiazepine hypnotics, its mechanism of action is to modulate subunits, especially the alpha-1 subunit, of the GABA receptor complex in order to induce sedation. Indiplon was developed in two different formulations to address two different types of insomnia complaint: indiplon-IR (immediate release) was designed for sleep onset difficulties, while indiplon-MR (modified release) was developed for sleep maintenance insomnia. While there are currently few peer reviewed articles about indiplon clinical trial results, the early information that is available seems to indicate that both formulations have been well tolerated and have proven effective at improving both patient reported and objectively measured sleep parameters in both adult and elderly insomnia patients. In May 2006, the FDA indicated that indiplon-IR was approvable and plans are to resubmit the application in 2007. Indiplon-MR was unapprovable and may require further evaluation.
Chemical Formula: C20H16N4O2S
Exact Mass: 376.0994
Molecular Weight: 376.43
Elemental Analysis: C, 63.81; H, 4.28; N, 14.88; O, 8.50; S, 8.52
Chemical Name: N-methyl-N-[3-[3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide
InChi Code: InChI=1S/C20H16N4O2S/c1-13(25)23(2)15-6-3-5-14(11-15)17-8-9-21-20-16(12-22-24(17)20)19(26)18-7-4-10-27-18/h3-12H,1-2H3
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
Shimizu M, Fukami T, Ito Y, Kurokawa T, Kariya M, Nakajima M, Yokoi T. Indiplon is hydrolyzed by arylacetamide deacetylase in human liver. Drug Metab Dispos. 2014 Apr;42(4):751-8. doi: 10.1124/dmd.113.056184. Epub 2014 Jan 24. PubMed PMID: 24464802.
Xu L, Wang J, Xiao B, Yang J, Liu Y, Huang R. Preparation and characterization of a novel polymorph of indiplon, Form α. Bioorg Med Chem Lett. 2012 Jan 15;22(2):963-8. doi: 10.1016/j.bmcl.2011.12.013. Epub 2011 Dec 9. PubMed PMID: 22209207.
Lemon MD, Strain JD, Hegg AM, Farver DK. Indiplon in the management of insomnia. Drug Des Devel Ther. 2009 Sep 21;3:131-42. PubMed PMID: 19920929; PubMed Central PMCID: PMC2769245.
Marrs JC. Indiplon: a nonbenzodiazepine sedative-hypnotic for the treatment of insomnia. Ann Pharmacother. 2008 Jul;42(7):1070-9. doi: 10.1345/aph.1K683. Epub 2008 Jul 1. PubMed PMID: 18594049.
Farber RH, Burke PJ. Post-bedtime dosing with indiplon in adults and the elderly: results from two placebo-controlled, active comparator crossover studies in healthy volunteers. Curr Med Res Opin. 2008 Mar;24(3):837-46. doi: 10.1185/030079908X273327. Epub 2008 Feb 6. PubMed PMID: 18257978.
Roth T, Zammit GK, Scharf MB, Farber R. Efficacy and safety of as-needed, post bedtime dosing with indiplon in insomnia patients with chronic difficulty maintaining sleep. Sleep. 2007 Dec;30(12):1731-8. PubMed PMID: 18246982; PubMed Central PMCID: PMC2276136.
Lankford A. Indiplon in the treatment of sleep disorders. Neuropsychiatr Dis Treat. 2007 Dec;3(6):765-73. PubMed PMID: 19300612; PubMed Central PMCID: PMC2656319.
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