As a GABA receptor agonist, magnesium stimulates GABA by binding to the GABA receptor and mimicking its actions. Magnesium also plays an important role in promoting GABA activity by blocking the NMDA receptor, an excitatory receptor that can cause anxiety and restlessness when overactive.

Yes, GABA and magnesium can be taken together to support relaxation and feelings of calm.

However, GABA supplements should not be confused with Gabapentin, a drug that is structurally related to GABA and used to prevent seizures in adults. In contrast to GABA, gabapentin readily penetrates the blood–brain barrier and rapidly increases GABA concentrations. There is a risk that magnesium may decrease how much gabapentin the body absorbs, which can then decrease the effects of gabapentin.

Yes, magnesium increases the activity of GABA receptors, making them more responsive. This enhances the calming effects of GABA in the brain without necessarily increasing the amount of GABA itself.

As well as magnesium, a number of other supplements have been shown to increase GABA activity in the brain:

• Key constituents in ashwagandha act as potent agonists of GABA receptors, which may explain its adaptogenic properties.
• Valerian may increase GABA concentrations and decrease central nervous system activity by inhibiting the enzymes that break down GABA. Valerian may also bind directly to GABA-A receptors, stimulating its release and reuptake.
• Taurine is a weak GABA agonist but has been shown to calm certain brain cells by activating specific receptors, similar to how GABA works. This suggests taurine might naturally help to regulate excitability in the thalamus, a key brain area.
• Safrana, an organic compound isolated from saffron, acts as an agonist on GABA receptors, increasing GABA activity.

Certain medications may be problematic when taken with magnesium. Magnesium can decrease the absorption and effectiveness of the following:

• Some antibiotics such as tetracycline, ciprofloxacin
• Some statin drugs such as atorvastatin (Lipitor)
• Anti-seizure drugs such as gabapentin (Neurontin)
• Thyroid medication levothyroxine (Synthroid)

Research suggests that magnesium and GABA may work together to help with relaxation and healthier sleep patterns. By binding to and activating GABA receptors, magnesium may increase GABA activity in the brain. GABA helps to counter excitatory neurotransmitters in the brain, reducing stimulation and helping you to feel more relaxed at bedtime and allowing you to fall asleep more easily.