What is Gamma Aminobutyric Acid (GABA) Discovery Synthesis Function Receptor Agonist and Antagonist

Gamma Aminobutyric Acid (GABA) is the major inhibitory neurotransmitter of the mammalian CNS. In humans, GABA is also directly responsible for the regulation of muscle tone. It is broadly distributed in the brain. Implicated in broad range of neuropsychiatric disorders like seizures, anxiety disorders, schizophrenia, alcohol dependence etc. 

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Discovery of Gamma Aminobutyric Acid

• In 19th century – was know as a metabolite of plant and microorganisms.
• In early 20th century - was isolated as an amino acid in the brain of mouse through paper chromatography. 
• In 1950 Robert and Frankel discovered GABA in human brain. 
• GABA patches: inhibitory effects
• Gamma- aminobutyric acid was first synthesized in 1883.
• In 1950, however, GABA was discovered to be an integral part of the mammalian central nervous system.

Synthesis of gamma aminobutryric acid

GABA does not penetrate the blood–brain barrier. it is synthesized in the brain. It is synthesized from glutamate using the enzyme L-glutamic acid decarboxylase (GAD) and vitamin B6.

GABA Synthesis

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Functions Of gamma aminobutyric acid

Functions of GABA

Pharmacology of Gamma aminobutyric acid

• Drugs that act as allosteric modulators of GABA receptors.
• Increase the available amount of GABA typically have relaxing, anti-anxiety, and anti-convulsive effects. 
• Many of the substances below are known to cause anterograde amnesia and retrograde amnesia.
• In general, GABA does not cross the blood–brain barrier.
• At least one study suggests that orally administered GABA increases the amount of Human Growth Hormone (HGH).
• GABA directly injected to the brain has been reported to have both stimulatory and inhibitory effects on the production of growth hormone, depending on the physiology of the individual.

Receptor of Gamma aminobutyric acid 

The GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. 

There are three classes of GABA receptors : 

1. GABA A Receptor
2. GABA B Receptor
3. GABA C Receptor 

GABA A receptors are ligand-gated ion channels (also known as ionotropic receptors) 

GABA B receptors are G protein-coupled receptors (also known as metabotropic receptors)

GABA C receptors A subclass of ionotropic GABA receptors, insensitive to typical allosteric modulators of GABA A receptor channels such as benzodiazepines and barbiturates,  was designated GABA С receptor.

Agonist and antagonist OF gamma amino butyric acid

Classification of gamma amino butyric acid A and Pharmacological action 

Classification of GABA A receptor with Pharmacological Effect

Advance Pharmacology Research On Gamma Aminobutyric Acid (GABA)

• New Insights Into The Role Of The GABA A—benzodiazepine Receptor In Psychiatric Disorder

Present current knowledge about the role of the GABA A—benzodiazepine receptor in anxiety disorders, new insights into the molecular biology of the receptor complex and neuro-imaging studies suggesting involvement of these receptors in disease states.

The molecular biology of this receptor is detailed. Molecular genetic studies suggesting involvement of the GABA A—benzodiazepine receptor in animal behavior and learning are outlined; possible parallels with human psychopathology are discussed.

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Current insights into the role of the GABA A—benzodiazepine receptor in the action of benzodiazepines and as a factor in disease states, in both animals and humans, may lead to new, more sophisticated interventions at this receptor complex and potentially significant therapeutic gains. present current knowledge about the role of the GABA A—benzodiazepine receptor in anxiety disorders, new insights into the molecular biology of the receptor complex and neuro-imaging studies suggesting involvement of these receptors in disease states.

The molecular biology of this receptor is detailed. Molecular genetic studies suggesting involvement of the GABA A—benzodiazepine receptor in animal behavior and learning are outlined; possible parallels with human psychopathology are discussed.

Current insights into the role of the GABA A—benzodiazepine receptor in the action of benzodiazepines and as a factor in disease states, in both animals and humans, may lead to new, more sophisticated interventions at this receptor complex and potentially significant therapeutic gains.

• Type 1 diabetes 'reversed' in human cells using GABA

In 2011, the team published a study demonstrating how injections of the amino acid gamma-aminobutryic acid (GABA) not only prevented mice from getting type 1 diabetes, but also reversed the disease in mice that already had the disease.

Scientists have known for decades that "GABA plays an important role in the brain as a neurotransmitter, where it facilitates the communication between nerve cells." 

However, its role in the pancreas - where it is produced - was not known until the 2011 paper.

In their latest research, the team trialed the therapy in mice that had been injected with human pancreatic cells. In the December issue of the journal Diabetes, they report that GABA has the same diabetes-reversing effect on the human cells that it did in the mice from the previous study.

• The role of GABA A receptors in mediating the effects of alcohol in the central nervous system

Ethanol is a chemically simple compound that produces many well-known effects in humans. The prevailing idea for many years was that ethanol and other alcohols exerted their effects on the central nervous system (CNS) by non-selectively disrupting the lipid bilayers of neurons. 

However, in recent years, there has been an accumulation of evidence pointing to the importance of ligand-gated ion channels (LGICs) in mediating the effects of ethanol. 

Of these LGICs, γ-aminobutyric acid type A (GABA A) receptors appear to occupy a central role in mediating the effects of ethanol in the CNS. 

GABA is the primary inhibitory neurotransmitter in the mammalian CNS, and activation of GABA A receptors by GABA tends to decrease neuronal excitability. 

This article reviews several aspects of GABA A receptor and ethanol interactions, including the evidence for short- and long-term modulation of GABA A receptors by ethanol and evidence for a GABA A receptor-related genetic component of alcoholism.

• The role of GABAergic system in neuro-developmental disorders: a focus on autism and epilepsy

Autism spectrum disorders (ASD) and epilepsy are very common neurological disorders of childhood, with an estimated incidence of about 0.5 – 1 % in worldwide population. 

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ASD and epilepsy are often associated, suggesting that common neurodevelopmental bases may exist for these two disorders. 

The neurodevelopmental bases of both ASD and epilepsy have been clearly showed by a number of genetic, neuroimaging and neuropathological studies.

In recent years, dysfunction of inhibitory GABAergic circuits has been proposed as a cause for both disorders.

Several studies performed on both animal models and postmortem human samples indicate that GABAergic neurons and circuits are altered in both ASD and epilepsy, suggesting- 

"The excitation/inhibition imbalance resulting from neurodevelopmental defects in GABAergic circuitry might represent a common pathogenetic mechanism for these disorders." 

Here, we will review the most significant studies supporting this hypothesis.