Role of catecholamines in the modafinil and amphetamine induced wakefulness, a comparative pharmacological study in the cat

Lin, Jian‐Sheng; Roussel, Bernard; Akaoka, H.; Fort, Patrice; Debilly, G.; Jouvet, Michel

doi:10.1016/0006-8993(92)91713-o

Cited by 191 publications

(128 citation statements)

References 27 publications

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“…Both tiprolisant and modafinil enhanced wakefulness during the lights-off (active) period in orexin-/-mice, as is observed in WT rodents (Scammell et al,2000;Parmentier et al,2007;Ligneau et al,2007b) and cats (Lin et al,1992;Ligneau et al,1998Ligneau et al, ,2007a.…”

Section: Discussionmentioning

confidence: 64%

“…We found that modafinil enhanced tMeHA levels to a lesser extent than tiprolisant and that it did not significantly affect MHPG/NA ratio. Similarly, modafinil-induced waking was accompanied with c-fos labeling in the tuberomammillary nucleus but not the locus coeruleus in rats (Scammell et al,2000) and its arousal-promoting action did not involve the presynaptic noradrenergic system in cats and mice (Lin et al,1992;Wisor and Eriksson, 2005). Nevertheless, the change in t-MeHA was of modest amplitude and the wake-promoting effect of modafinil is unaffected in mice KO for the gene of the HA-synthesizing enzyme (Parmentier et al,2007).…”

Section: Discussionmentioning

confidence: 96%

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An inverse agonist of the histamine H3 receptor improves wakefulness in narcolepsy: Studies in orexin−/− mice and patients

Lin

Dauvilliers

Arnulf

et al. 2008

Neurobiology of Disease

247

178

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Abbreviations AbstractNarcolepsy is characterized by excessive daytime sleepiness(EDS), cataplexy, direct onsets of rapid eye movement(REM) sleep from wakefulness(DREMs) and deficiency of orexins, neuropeptides that promote wakefulness largely via activation of histamine (HA) pathways. The hypothesis that the orexin defect can be circumvented by enhancing HA release was explored in narcoleptic mice and patients using tiprolisant, an inverse H3-receptor agonist. In narcoleptic orexin-/-mice, tiprolisant enhanced HA and noradrenaline neuronal activity, promoted wakefulness and decreased abnormal DREMs, all effects being amplified by co-administration of modafinil, a currently prescribed wake-promoting drug. In a pilot single-blind trial on 22 patients receiving a placebo followed by tiprolisant, both for one week, the Epworth Sleepiness Scale(ESS) score was reduced from a baseline value of 17.6 by 1.0 with the placebo(p>0.05) and 5.9 with tiprolisant(p<0.001). Excessive daytime sleep, unaffected under placebo, was nearly suppressed on the last days of tiprolisant-dosing. H3-receptor inverse agonists could constitute a novel effective treatment of EDS, particularly when associated with modafinil.

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Section: Discussionmentioning

confidence: 64%

Section: Discussionmentioning

confidence: 96%

An inverse agonist of the histamine H3 receptor improves wakefulness in narcolepsy: Studies in orexin−/− mice and patients

Lin

Dauvilliers

Arnulf

et al. 2008

Neurobiology of Disease

247

178

View full text Add to dashboard Cite

show abstract

“…Its mechanism of action is not completely understood but is believed to work through its action on brain GABA levels. Modafinil lowers brain GABA concentration indirectly by stimulating the noradrenergic system to activate serotoninergic neurones, which inhibit the release of GABA [31,32,33]. Both the noradrenergic and serotoninergic systems are involved in memory processing and cognition [34,35].…”

Section: Discussionmentioning

confidence: 99%

The effect of modafinil on counter-regulatory and cognitive responses to hypoglycaemia

et al. 2004

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Aims/hypothesis. Our hypothesis is that reducing release of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) with modafinil will enhance symptomatic and hormonal responses to hypoglycaemia. Methods. Nine healthy men received, in random order, two 100-mg doses of modafinil or placebo, followed by an insulin clamp in which plasma glucose was either reduced stepwise to 2.4 mmol/l or was sustained at euglycaemia (four studies). Catecholamines, symptom scores and cognitive function were measured. Results. Modafinil had no effect on the measured parameters during euglycaemia. During hypoglycaemia, autonomic symptom scores were significantly higher with modafinil (increase at lowest plasma glucose concentration 271.3±118.9 vs 211.2±80.4/40 min, p=0.019), and the heart rate response was increased (12,928±184 vs 6773±148 bpm/140 min, p=0.016). Deterioration in performance of two cognitive tasks was reduced: Stroop colour-word test (613±204 vs 2375±161/65 min, p=0.009) and accuracy of a simple reaction task (11.3±1.8 vs 9.4±3.7, p=0.039). Conclusions/interpretation. We conclude that modafinil improves adrenergic sensitivity and some aspects of cognitive function at hypoglycaemia, possibly by reducing neuronal central GABA concentrations.

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“…In support of this assumption, one of the few genes in the rat brain which is significantly induced and proportionally expressed after sleep deprivation is that of arylsulfotransferase, a final enzyme responsible for the catabolism of catecholamines in rodents [39; 40]. Thus the absence of sleep rebound associated with modafinil could also be interpreted as absence of catecholamine exhaustion as the waking effect of modafinil does not seem to depend on endogenous catecholamines [35]. Moreover, no signs of direct neuronal depolarization/excitation on target cells have been reported for modafinil, even though diffuse expression of immediate early gene c-fos [41], or enhanced histamine release [42] occurred with high doses of modafinil.…”

Section: Absence Of Sleep Reboundmentioning

confidence: 99%

The brain H3-receptor as a novel therapeutic target for vigilance and sleep–wake disorders

Parmentier

Anaclet

Guhennec³

et al. 2007

Biochemical Pharmacology

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Role of catecholamines in the modafinil and amphetamine induced wakefulness, a comparative pharmacological study in the cat

Cited by 191 publications

References 27 publications

An inverse agonist of the histamine H3 receptor improves wakefulness in narcolepsy: Studies in orexin−/− mice and patients

An inverse agonist of the histamine H3 receptor improves wakefulness in narcolepsy: Studies in orexin−/− mice and patients

The effect of modafinil on counter-regulatory and cognitive responses to hypoglycaemia

The brain H3-receptor as a novel therapeutic target for vigilance and sleep–wake disorders

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