Eugeroic

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Eugeroic
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A eugeroic, or eugregoric, is a type of

psychostimulants.[1] However, the term "eugeroic" has not been widely adopted in the literature, and instead the term "wakefulness-promoting agent" (and variations thereof) has been more widely used, both for modafinil-type drugs and other agents.[1][8][9][10]

Eugeroics, in the sense of modafinil-type wakefulness promoting agents, include modafinil itself,

misuse potential.[3][4][12]

Modafinil and armodafinil are thought to act as selective, weak, atypical dopamine reuptake inhibitors (DRIs).[13][3][4] However, additional actions are also possible and have not been ruled out.[13] Adrafinil acts as a prodrug of modafinil and hence shares its mechanism of action.[13] Certain other drugs acting as atypical DRIs with known or potential wakefulness-promoting effects include solriamfetol (also a norepinephrine reuptake inhibitor),[14][15] vanoxerine,[16] phenylpiracetam,[17][18][19] and mesocarb.[20][21][22][23] Other wakefulness-promoting agents act in a variety of other ways.[16][1][10][24]

List of eugeroics

Marketed

Discontinued

  • Adrafinil (Olmifon, CRL-40028, N-hydroxymodafinil) – a hydroxy-substituted derivative and prodrug of modafinil

Never marketed

  • Esmodafinil (CRL-40983, (S)-modafinil) – the (S)-enantiomer of modafinil
  • Fladrafinil (CRL-40941, fluorafinil, bisfluoroadrafinil) – a bisfluoro-substituted derivative of adrafinil
  • Flmodafinil (CRL-40940, NLS-4, JBG01-41, bisfluoromodafinil, lauflumide) – a bisfluoro-substituted derivative of modafinil
  • Fluorenol ("hydrafinil") – a novel eugeroic structurally unrelated to modafinil and its analogues
  • Modafiendz (methylbisfluoromodafinil) – a methyl and bisfluoro-substituted derivative of modafinil

Novel eugeroics

See also: List of modafinil analogues and derivatives

The

motivational disorders.[27][28][29][17]

References

  1. ^
    PMID 38852786
    .
  2. ISSN 1080-563X
    .
  3. ^ a b c d "Provigil: Prescribing information" (PDF). United States Food and Drug Administration. Cephalon, Inc. January 2015. Retrieved 16 August 2015.
  4. ^ a b c d "Nuvigil: Prescribing information" (PDF). United States Food and Drug Administration. Cephalon, Inc. April 2015. Retrieved 16 August 2015.
  5. PMID 32447354
    .
  6. PMID 37590820
    .
  7. PMID 8904200
    .
  8. PMID 15532213
    .
  9. ^
    PMID 25312027
    .
  10. ^
    PMID 37082610
    .
  11. ^ "Practice Parameters for the Treatment of Narcolepsy and other Hypersomnias of Central Origin" (PDF). American Academy of Sleep Medicine (AASM). September 2007.
  12. S2CID 40801601
    .
  13. ^
    PMID 38467484
    .
  14. ISSN 2198-6401
    .
  15. PMID 31215815
    .
  16. ^
    ISBN 978-3-319-23738-1
    .
  17. ^
    PMID 37788571
    .
  18. ISSN 0009-3122
    . Phenylpiracetam was originally designed as a nootropic drug for the sustenance and improvement of the physical condition and cognition abilities of Soviet space crews.2 Later, especially during the last decade, phenylpiracetam was introduced into general clinical practice in Russia and in some Eastern European countries. The possible target receptors and mechanisms for the acute activity of this drug remained unclear, until very recently it was found that (R)-phenylpiracetam (5) (MRZ-9547) is a selective dopamine transporter inhibitor that moderately stimulates striatal dopamine release.19
  19. PMID 24964269
    . Here, we tested the effects of MRZ-9547 [...], and its l-enantiomer MRZ-9546 on effort-related decision making in rats. The racemic form of these compounds referred to as phenotropil has been shown to stimulate motor activity in rats (Zvejniece et al., 2011) and enhance physical capacity and cognition in humans (Malykh and Sadaie, 2010). [...] MRZ-9547 turned out to be a DAT inhibitor as shown by displacement of binding of [125I] RTI-55 (IC50 = 4.82 ± 0.05 μM, n=3) to human recombinant DAT expressed in CHO-K1 cells and inhibition of DA uptake (IC50 = 14.5 ± 1.6 μM, n=2) in functional assays in the same cells. It inhibited norepinephrine transporter (NET) with an IC50 of 182 μM (one experiment in duplicate). The potencies for the l-enantiomer MRZ-9546 were as follows: DAT binding (Ki = 34.8 ± 14.8 μM, n=3), DAT function (IC50 = 65.5 ± 8.3 μM, n=2) and NET function (IC50 = 667 μM, one experiment performed in duplicate).
  20. PMID 36935752
    .
  21. PMID 38836245
    .
  22. PMID 34199621
    .
  23. ISBN 978-1-315-37366-9. Finally, [mesocarb] promotes wakefulness and therefore is anticipated to address the excessive daytime sleepiness (EDS) associated with PD (Mitler et al. 2000; Gjerstad et al. 2002; Larsen 2003; Arnulf 2005; Lökk 2010), which is a significant unmet medical need in this patient population. Melior's further investigations showed that the therapeutic activity described here was greatest when administering optimal dose levels of the active l-enantiomer (MLR-1019 [armesocarb]) compared to optimal dose levels of the racemic mixture (sydnocarb).{{cite book}}: CS1 maint: location (link
    )
  24. PMID 32032921
    .
  25. PMID 22264475
    .
  26. ^
    PMID 22546675
    .
  27. PMID 34121988
    .
  28. PMID 32927246
    .
  29. PMID 36928847. {{cite book}}: |journal= ignored (help
    )
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