THE GABA-A RECEPTOR
A MAJOR THERAPEUTIC CHANNEL

THE GABAA 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.
“This whole area of GABA-A-active steroids is really new. 20 years ago nobody even knew about Allopregnanolone and its effect on GABA-A receptor mediated actions in the brain, so a lot has happened. Today there are several different research groups working with these kinds of substances, I’m hopeful more research will keep being carried out.”
Professor Marie Bixo, University of Umeå.