GABAARs and Effect of Phytocannabinoids on GABAergic Transmission

What is GABAARs GABAA Receptors ? 

GABAARs (Gamma γ-Aminobutyric acid type A receptors ) are the receptors and mediatory inhibitors ( Ligand-gated ion channel) in the plasma membrane of neurons located in the limbic area of the brain, primarily responsible for Feelings and Emotions, they play mediating role during the nerve impulse transmission ( Neurotransmission )and any mutation in them can cause like Epilepsy, Anxiety and other Neurological and Neurodevelopmental Diseases. They are divided into various isotypes assembled in a set of 19 subunits. 

How do GABA works? 

The inhibitory function is mediated by chloride ion movement across the GABAARs, activated by synaptic GABA release, reducing neuronal excitability in the adult CNS (Central Nervous System ). Several studies highlighted the importance of GABA – mediated transmission during neurodevelopment.


Effects of Phytocannabinoids & Drugs on GABAARs Receptors : 

Different classes of drugs can modulate the GABAARs function ( benzodiazepines, barbiturates, neurosteroids, alcohol ), up to now little is known about GABAARs and cannabinoids’ interaction in the CNS (Central Nervous System ). Endocannabinoids and phytocannabinoids are lately emerging as a new class of promising drugs for a wide range of neurological conditions, but their safety as medication and their mechanisms of action are still to be fully explained.


In this review, we will focus our attention on two of the most promising molecules ( A9 tetrahydrocannabinol: 19 – THC and cannabidiol; CBD ) of this new class of drugs and their possible mechanism of action on GABA Rs.

GABAARs and Effect of Phytocannabinoids on GABAergic Transmission