Neurotransmitters are chemical messengers that transmit and modulate signals from neurons to other cells of the brain and body across a synapse. When a neurotransmitter binds to its corresponding receptor, it activates or inhibits the receptor's associated pathway.
GABA, the most prevalent inhibitory neurotransmitter in the mammalian central nervous system, plays an essential role in regulating vital neurological functions. GABA’s natural function is to reduce the activity of the neurons to which it binds through GABA receptors (GABARs).
Regulation of both excitatory and inhibitory synaptic transmission is critical for proper nervous system function. GABARs are promising drug targets for a wide spectrum of psychiatric and neurological disorders. They are involved in sedative and anxiolytic activities.
Enhancement of GABA signaling has been demonstrated in patients with central nervous system hypersomnias. GABA-ergic disturbances are hallmark features of schizophrenia and other neuropsychiatric disorders.
GABA-ergic system has been associated consistently with atypicalities in autism and aggressive behavior. Modulators of the GABARs may be useful in the treatment of visual, sleep, and cognitive disorders.
GABARs have been associated with seizures and memory dysfunction when disrupted. The up-regulations of GABA in the brain may lead to an antiepileptic effect. The cerebellar cortex, the brain region responsible for motor coordination and learning expresses a high density of GABARs.
Repeated alcohol exposure during the third trimester of pregnancy increases expression of GABARs in cerebellar granule neurons and delays motor development in rats. Ethanol significantly reduces the brain metabolism, probably via action at specific GABARs. These receptors an important role in the neuroprotective effects of anthocyanins against ethanol.
Interestingly, increased expression of GABARs has been detected in several human cancer cells and tissues.
It was demonstrated that the absence of functional GABARs disturbs glucose homeostasis in mice.
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