GTS-21

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GTS-21 (also known as DMXB-A) is a synthetic compound that acts as a partial agonist at nicotinic acetylcholine receptors. It has been researched for its potential therapeutic uses in conditions such as Alzheimer's disease, schizophrenia, and neuroinflammation.

Chemistry[edit | edit source]

GTS-21 is a derivative of anabaseine, a naturally occurring substance found in certain species of Nicotiana (tobacco) plants. It is classified as a partial agonist, meaning it binds to and activates a receptor but not to its full capacity, allowing it to modulate the receptor's activity.

Pharmacology[edit | edit source]

GTS-21 selectively targets the α7 subtype of the nicotinic acetylcholine receptor (nAChR). This receptor subtype is found in the brain and other tissues and is involved in a variety of physiological processes. By acting as a partial agonist, GTS-21 can enhance the activity of these receptors, potentially offering therapeutic benefits in conditions where their function is impaired.

Clinical Research[edit | edit source]

Research into the potential therapeutic uses of GTS-21 has focused on conditions such as Alzheimer's disease and schizophrenia, where dysfunction of the α7 nAChR is thought to play a role. Studies have shown that GTS-21 can improve cognitive function in animal models of these conditions, and early-phase clinical trials in humans have shown promising results.

In addition to its potential neuroprotective effects, GTS-21 has also been studied for its anti-inflammatory properties. It has been found to reduce the production of pro-inflammatory cytokines, suggesting it may have potential as a treatment for conditions involving neuroinflammation.

Safety and Tolerability[edit | edit source]

GTS-21 has been found to be well-tolerated in clinical trials, with few adverse effects reported. However, as with any drug, further research is needed to fully understand its safety profile.

See Also[edit | edit source]

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Contributors: Prab R. Tumpati, MD