N-ArachidonylGABA is primarily studied for its role in modulating neurotransmitter activity in the central nervous system. It acts as a dual-acting compound, combining features of an endocannabinoid and a GABAergic agent. This unique structure allows it to influence both cannabinoid receptors and GABA transporters, making it a focus in research on neuroprotection and neuronal signaling.

It has shown potential in reducing neuronal excitability, suggesting possible applications in managing conditions like epilepsy, neuropathic pain, and other disorders involving overactive neural pathways. Due to its ability to inhibit GABA uptake, it may enhance inhibitory neurotransmission, which can help restore balance in excitatory-inhibitory signaling.

Research also explores its anti-inflammatory and analgesic properties, particularly in models of chronic pain and neurodegenerative diseases. Because it can cross the blood-brain barrier more effectively than some related compounds, it is considered a promising candidate for developing therapeutics targeting brain disorders.

Its activity in the endocannabinoid system further supports investigation into mood regulation, anxiety, and addiction pathways. While still in preclinical stages, N-ArachidonylGABA represents a novel approach in designing lipid-based neuromodulators with multitarget mechanisms.