How Modafinil Works in the Brain to Treat Sleep Disorders
Modafinil is used to treat narcolepsy and obstructive sleep apnea/hypopnea syndrome. It can also improve your thinking skills and work performance.
It’s becoming increasingly popular for healthy people to take modafinil as a ‘cognitive enhancer’. They do so without a prescription, and may put themselves at risk of adverse side effects.
Neurotransmitters
Buy Modafinil Online activates certain types of nerve cells that rely on the chemical signal glutamate to convey their nerve messages. These so-called glutaminergic nerve cells promote wakefulness. Modafinil also inhibits the function of another neurotransmitter called gamma-aminobutyric acid, or GABA. The function of GABA is to end nerve signals and relax nerve cells after they’ve sent a message.
When a nerve cell receives a nerve message, it triggers the release of chemicals from small sacs inside the nerve cell (called vesicles). These chemical signals are released at the point where two nerve cells meet, a junction called a synapse. The neurotransmitters then travel across the synapse and bind to receptors on connected nerve cells.
Studies using resting state fMRI have shown that people with insomnia exhibit impaired connectivity of the locus coeruleus to the orbitofrontal cortex, insula, precuneus, and anterior cingulate cortex (285). Moreover, gene-set analysis of specific brain tissue structures found that alterations in the sleep promoting neurotransmitter norepinephrine (or NE) are associated with risk for insomnia (314).
Glutamatergic Nerve Cells
Glutamate (or glutamic acid) is the principal excitatory neurotransmitter in the vertebrate brain and spinal cord, responsible for more than 90% of all synaptic connections. It controls cognitive functions, like thinking and learning, and also influences mood, sleep-wake cycles and pain transmission. Imbalances in glutamate have been implicated in a variety of neurodevelopmental and adult mental disorders, including autism spectrum disorders, substance abuse, and psychiatric illnesses.
Modafinil (Modalert 200 mg) increases the activity of glutamate neurons, and enhances the transmission of their signals. This effect is mediated by modulation of various receptors and transporters.
There are at least 30 proteins at, or near, the glutamate synapse that control, modulate, or interact with it (think of a master key that fits into and works four different partner locks). Two families of ionotropic receptors, NMDA and AMPA, and the metabotropic receptor kainate, all have ion channels that open when glutamate binds. These receptors are located at postsynaptic nerve cell terminals.
GABA Nerve Cells
GABA (gamma-aminobutryic acid) is an inhibitory neurotransmitter that lessens the ability of a nerve cell to receive, create or send chemical messages. GABA is known to produce a calming effect and helps control anxiety, stress, fear, and depression.
GABA is released by astrocytes and interneurons, and it regulates the balance between excitation and inhibition in neural circuits. It also controls the migration of neurons from the subventricular zone and cortical layers.
Astrocytes express functional GABAA receptors (GABA-r) that are coupled to voltage-gated calcium channels. Activation of these receptors induces chloride efflux and depolarization of astrocytes. This triggers the release of gliotransmitters that fine-tune synaptic communication.
Researchers have found that GABA plays a role in sleep maintenance. In one study, a drug that enhances GABA function helped increase the amount of slow-wave sleep and non-rapid eye movement sleep in mice. In addition, supplemental GABA has been shown to promote relaxation and alleviate stress and anxiety. This is thought to be because a balanced level of GABA reduces stress-related hormones and allows the body to process information more effectively.
Dopamine Nerve Cells
Dopamine is a neurotransmitter that helps nerve cells send messages to other cells in the brain. It plays an important role in feelings of pleasure, arousal and motivation as well as memory, movement, learning and concentration. Diseases associated with dopamine imbalance include Parkinson’s disease, schizophrenia, depression and restless legs syndrome. Drugs that block the pump that removes (or reuptakes) dopamine from the synapse help restore balance to these functions.
Modafinil has been shown to improve wakefulness in sleep disorders such as narcolepsy, obstructive sleep apnea and shift work sleep disorder. It is also being evaluated for its potential to reduce fatigue in Charcot-Marie-Tooth disease (CMT).1