Modafinil is a GABA Receptor Modulator

Modafinil Australia, marketed under the trade names Provigil and Nuvigil, is a highly effective wake-promoting agent. It acts in a unique way compared to traditional psychostimulants because it does not increase dopamine levels, is not associated with abuse potential and does not induce cataplexy in narcolepsy patients.

It binds competitively to the cell-membrane monoamine transporters (DAT, noradrenaline (NE), and serotonin (5-HT)). This displaces ligands from the transporters, thereby inhibiting their reuptake and enhancing neurotransmitter release.

Furthermore, modafinil enhances the release of 5-HT, norepinephrine and dopamine by increasing the availability of metabolic substrates through its inhibition of CYP2C9. This is likely to bolster neurotransmitter release via an increase in cellular metabolism and reduced free-radicals within neurons. However, these mechanisms do not adequately explain how modafinil promotes wakefulness and improves cognitive performance without affecting neurotransmitter levels or increasing glutamate in the brain.

Modalert is a GABA Inhibitor

Modalert is FDA-approved for the treatment of narcolepsy and obstructive sleep apnea. The drug is a powerful stimulant that is known as a “nootropic,” meaning it helps increase focus and alertness. The drug is available in different dosages and brands, including Modalert, Modvigil, Waklert, and Artvigil.

One way that modalert promotes wakefulness is by inhibiting GABA (gamma-aminobutyric acid). GABA is the primary inhibitory neurotransmitter in the brain, and modulating its activity leads to an increase in vigilance and alertness. Modalert also increases the release of glutamate, an excitatory neurotransmitter that stimulates neurons and improves cognitive function.

In addition, modalert tablet blocks dopamine transporter (DAT) and increases the concentration of dopamine in the synaptic cleft. This increase in dopamine stimulates postsynaptic dopamine receptors and enhances the activation of arousal systems. In microdialysis studies, it has been shown that a vigilance enhancing dose of modafinil reduces local extracellular GABA levels in the medial preoptic area (MPA) and posterior hypothalamus (PH), suggesting that GABA transmission is important for regulating the sleep-wake cycle.

Modalert is a Serotonin Reuptake Inhibitor

Modafinil is a wakefulness-promoting drug used to treat excessive sleepiness in narcolepsy and shift work sleep disorder. It is also used by some healthy people to boost alertness and focus. It is a member of the class of psychostimulants and shares many features with amphetamine, but it has a different mechanism of action.

Modalert does not directly bind to the DA receptor, but does increase the stimulation of TA1 in cells expressing both DAT and NET. It also interacts with orexin neurons to promote wakefulness. Modafinil induces Fos-immunoreactivity in orexin neurons in the perifornical region of the brain, and it increases wakefulness when administered to orexin deficient mice. It also enhances the effects of the DA autoreceptor antagonists terazosin and quinpirole.

Modafinil also potentiates the increase of extracellular serotonin levels induced by the antidepressants fluoxetine and imipramine in brain regions of the awake rat, suggesting another neurochemical action of this drug. It also enhances the amplitude of the increase in cortical serotonin released by the selective a2 agonist yohimbine, indicating that a combination of pre- and postsynaptic actions may contribute to its behavioral effects.

Modalert is a Serotonin Reuptake Enhancer

Modalert affects various receptors in the brain, causing it to increase wakefulness and reduce excessive daytime sleepiness. It also acts as a dopamine reuptake inhibitor, blocking the reuptake of the neurotransmitter dopamine from brain terminals. This increases the levels of DA in the brain, which is associated with increased alertness and cognitive performance.

Studies have shown that MOD enhances the synchronization of cortical neurons, thalamic reticular neurons, and subcoerulear nucleus neurons. It also increases the amplitude of evoked potentials in the suprachiasmatic nucleus, which is associated with increased alertness and improved cognitive function.

These properties make MOD a promising candidate for use as an adjunct therapy for mental illnesses that impair cognition, such as schizophrenia and bipolar disorder. It is also a useful wakefulness-promoting agent for military personnel, who experience periods of sleep deprivation frequently. MOD has low, if any, abuse liability and is less likely to cause significant adverse effects on cognition than typical psychostimulants.