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Other names | 3-(2,4-dimethoxy-benzylidene)anabaseine |
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Formula | C19H20N2O2 |
Molar mass | 308.381 g·mol−1 |
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![]() | This article needs to be updated.(April 2015) |
GTS-21 (DMXBA or DMBX-anabaseine) is a drug has been ability to potentially enhance memory and cognitive function. It has been studied for its potential therapeutic uses, particularly in the treatment of neurodegenerative diseases and psychiatric disorders.
It is a derivative of the natural product anabaseine that acts as a partial agonist at neural nicotinic acetylcholine receptors (nAChRs). It binds to both the α4β2 and α7 subtypes, but activates only the α7 to any significant extent. [1] [2] Activation of the α7 nAChR has been shown to have neuroprotective effects and to improve cognitive function, making it an attractive target for drug development.
Both GTS-21 itself and its demethylated active metabolite 4-OH-GTS-21 [3] display nootropic [4] and neuroprotective effects, [5] [6] [7] [8] and GTS-21 is being investigated for the treatment of Alzheimer's disease, [9] [10] nicotine dependence, [11] and, most significantly, for schizophrenia. [12] [13] [14] [15] [16]
Several studies have investigated the effects of GTS-21 in various animal models of neurodegenerative diseases, including Alzheimer's disease, Parkinson's disease, and multiple sclerosis. In these studies, GTS-21 has been shown to have anti-inflammatory and neuroprotective effects, and to improve cognitive function.
A recent study investigated the cholinergic anti-inflammatory pathway (CAP) in rheumatoid arthritis (RA). They used the α7 nicotinic acetylcholine receptor (α7nAChR) agonist GTS-21 to study its role in reducing synovial inflammation in a mice model of collagen-induced arthritis (CIA). GTS-21 lessened inflammation and reduced monocyte infiltration into the synovium. This study highlights a new mechanism by which cholinergic signaling can mitigate synovial inflammation in RA. [17]
Phase one of a clinical trial using DXMBA as a potential treatment for schizophrenia was completed in January of 2005. [18] This clinical trial untimely was discontinued during phase II. [18] Several other trials focusing on a range of health issues including Alzheimer's, schizophrenia, autism, ADHD, and nicotine use were either discontinued or withdrawn. [19] [20] [21] [22] [23]
Another study of GTS-21 in healthy volunteers found that the drug improved attention and memory performance. [4]
The laboratory name GTS-21 means that it is the 21st chemical compound created by Gainesville (University of Florida in Gainesville) and Tokushima (Taiho Pharmaceutical) Scientists. [24] DMXBA – 3-2,4-dimethoxybenzylidene anabaseine.