REVIEW Adrafinil (CRL-40028, Olmifon), prodrug of modafinil, is a mild central nervous system stimulant drug used to relieve excessive sleepiness and inattention, Adrafinil is believed to serve as an alpha-1 adrenoceptor agonist. IC50 value: Target: in vitro: in vivo: CRL 40028 antagonizes prazosin-induced hypothermia and hypomotility; prazosin antagonizes the anticonvulsant effect of CRL 40028 in the quaking mouse. Adrafinil in rat serum was stable over three freeze-thaw cycles at ambient temperature for 6 h. The method had a lower limit of quantitation of 16.5 ng/ml, which offered high sensitivity for the determination of adrafinil in serum. Aged beagle dogs were trained on either a size or intensity discrimination task 2 h following treatment with either 20 mg/kg of adrafinil or a placebo control. Treatment with adrafinil produced significant improvement in learning, as indicated by a decrease in both errors and trials to criterion. An effect of adrafinil on motivation may partially account for these findings; however, adrafinil did not significantly affect response latency. Adrafinil is believed to serve as an alpha-1 adrenoceptor agonist.
REFERENCES
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Milgram NW, et al. Oral administration of adrafinil improves discrimination learning in aged beagle dogs. Pharmacol Biochem Behav. 2000 Jun;66(2):301-5.
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Rao RN, et al. LC-ESI-MS determination and pharmacokinetics of adrafinil in rats. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Sep 15;873(1):119-23.
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Simon P, et al. Pharmacological evidence of the stimulation of central alpha-adrenergic receptors. Prog Neuropsychopharmacol Biol Psychiatry. 1983;7(2-3):183-6.
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