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CRL-40,940 (also known as flmodafinil, bisfluoromodafinil, NLS-4, and lauflumide) is the bisfluoro analog of modafinil.[1][2][3][4] It is a eugeroic as well as a weak dopamine reuptake inhibitor. Its inventors claim that it is more effective than modafinil and adrafinil, with fewer side effects. It was patented in 2013, and pre-clinical trials have been underway since December 2015.[5]

Pre-clinical research

In a study comparing the wake-promoting effects of NLS-4 and modafinil, NLS-4 was found to maintain wakefulness over a significantly longer timeframe than modafinil. While the administration of neither compound resulted in sleep rebound, NLS-4 perturbed sleep architecture to a lesser degree than modafinil. This difference was characterised by an attenuated EEG power density within slow frequencies (<4Hz) following NLS-4 treatment, though both compounds increased power density relative to placebo.[6]

See also

References

  1. ^ CA 1199916, Lafon L, "Benzhydrylsulfinylacetamide derivatives", published 28 January 1986, issued 28 January 1986, assigned to Cephalon France SAS 
  2. ^ Cao J, Prisinzano TE, Okunola OM, Kopajtic T, Shook M, Katz JL, et al. (October 2010). "Structure-Activity Relationships at the Monoamine Transporters for a Novel Series of Modafinil (2-[(diphenylmethyl)sulfinyl]acetamide) Analogues". ACS Medicinal Chemistry Letters. 2 (1): 48–52. doi:10.1021/ml1002025. PMC 3041981. PMID 21344069.
  3. ^ US 20130295196, Konofal E, "Lauflumide and the enantiomers thereof, method for preparing same and therapeutic uses thereof", published 7 November 2013, issued 2 May 2017, assigned to NLS Pharmaceutics AG and Assistance Publique Hopitaux de Paris APHP 
  4. ^ US 4489095, Lafon L, "Halogenobenzhydrylsulfinylacetohydroxamic acids", issued 18 December 1984, assigned to Cephalon France SAS 
  5. ^ "Pipeline". NLS Pharmaceuticals.
  6. ^ Luca G, Bandarabadi M, Konofal E, Lecendreux M, Ferrié L, Figadère B, et al. (2018-08-15). "Lauflumide (NLS-4) Is a New Potent Wake-Promoting Compound". Frontiers in Neuroscience. 12: 519. doi:10.3389/fnins.2018.00519. PMC 6104159. PMID 30158846.
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