THE GABA-A RECEPTOR
A MAJOR THERAPEUTIC CHANNEL
Neurosteroids are some of the body’s most powerful, high-impact compounds. They exert huge influence over our lives, modulating our emotions, reward and pleasure centers, and emotional, cognitive and memory functions. But which compounds modulate them? A new generation of highly specific therapeutic compounds can now potentially “modulate the modulators” and “control the controllers”. They too operate within the GABA-A receptors—the brain’s major inhibitory signaling system, and a fast-emerging therapeutic channel.
NEUROSTEROIDS AND GABA-A RECEPTORS
Allopregnanolone, THDOC, Androstanediol and Pregnanolone—few have heard of them, yet they are powerful neurosteroids with a major impact on all of us.
Synthesized in both the brain and endocrine glands, these potent neurochemicals enter our bloodstream and affect our brain functions, producing a wide range of effects ranging from stress- and anxiety- reduction to analgesia and sedation but can also, in diseased individuals, cause the opposite effects. The neurosteroids are highly active within, and primarily target, the brain’s GABA-A receptors.
GABA-A RECEPTORS: WHAT AND WHERE THEY ARE
The major action for GABA within the brain, GABA-A receptors, are chloride channels that are opened, closed and modulated by the chemical action of neurosteroids.
GABA-A receptors exist in several subtypes with specific location in the brain related to the function of the brain area. For example, within the brain’s limbic system – the area of the brain where personal feelings, emotions and memories are generated and stored. GABA-A receptors of different types exist within the amygdala, the thalamus and the hippocampus.
A MAJOR THERAPEUTIC CHANNEL
Over the last 20 years, the GABA-A receptor has been at the center of a fast-emerging research field of great pharmaceutical potential.
Groundbreaking research has been carried out into the receptor, the potent neurosteroids that influence it, and a newly discovered group of highly targeted modulating compounds that in turn impact those neurosteroids.
These compounds have been named GAMSAs (GABA-A Modulating Steroid Antagonists).
Asarina Pharma’s Founder and CSO Prof Torbjörn Bäckström is one of the world’s preeminent and pioneering researchers into the GABA-A receptor and GAMSAs.