GTS-21 HCl

Description

GTS-21 HCl
CAS Number	156223-05-1
Molar Mass	381.30 g/mol
Chemical Formula	C19H22Cl2N2O2
IUPAC Name	3-[(5E)-5-[(2,4-dimethoxyphenyl)methylidene]-3,4-dihydro-2H-pyridin-6-yl]pyridine dihydrochloride

Introduction

GTS-21 HCl is a synthetic anabaseine derivative and small molecule research compound supplied strictly for laboratory and in vitro use. It is studied by researchers investigating alpha7 nicotinic acetylcholine receptor signaling, cholinergic anti-inflammatory pathways, and cognitive function. GTS-21 is not intended for human consumption, veterinary use, or any application outside of a controlled research setting.

Key Characteristics

GTS-21 HCl is manufactured to a high standard of chemical purity to support reproducible research outcomes. Each batch is formulated with attention to structural precision and lot-to-lot consistency, allowing researchers to rely on stable results across independent experiments.

Research Applications

GTS-21 is used in immunology, neuropharmacology, and cognitive research to investigate alpha7 nicotinic acetylcholine receptor-mediated signaling. It serves as a selective partial agonist tool for probing how this receptor pathway relates to inflammatory cytokine regulation, hippocampal neuronal survival, and measures of attention and memory in model systems and research participants.

Research Benefits

GTS-21 and Inflammatory Cytokine Regulation

Research indicates that GTS-21 dose-dependently inhibits tumor necrosis factor and high mobility group box 1 release, along with nuclear factor-kappaB activation, in cultured macrophages exposed to endotoxin. Studies have investigated this mechanism in animal models of endotoxemia and severe sepsis, finding that GTS-21 administration significantly reduced serum levels of these inflammatory mediators and improved survival outcomes.

GTS-21 and Cognitive Performance

Studies propose that GTS-21 supports measures of attention, working memory, and episodic secondary memory. Researchers use this model to explore how alpha7 nicotinic receptor activation relates to cognitive performance, with a randomized, double-blind clinical trial in healthy male volunteers finding statistically significant enhancement across these three cognitive measures compared to placebo, with a dose-related relationship between drug exposure and the magnitude of the response.

GTS-21 and Hippocampal Neuroprotection

Research suggests that GTS-21 pretreatment attenuates neuronal apoptosis and preserves neuronal density in the hippocampal CA1 region following exposure to inhalation anesthesia in aged animal models. Studies have investigated this mechanism alongside reductions in hippocampal interleukin-1 beta expression, finding that GTS-21 pretreatment was associated with preserved spatial learning and memory performance compared to untreated aged animals.

Summary

GTS-21 HCl is a synthetic anabaseine derivative supplied exclusively for laboratory research. It supports investigation into three distinct areas: inflammatory cytokine regulation, cognitive performance, and hippocampal neuroprotection. As with all research compounds in this catalog, GTS-21 is intended strictly for research use and not for human or veterinary application.

Disclaimer

This content is presented exclusively for educational purposes and should not be construed as medical advice. THE MATERIALS REFERENCED HEREIN ARE EXCLUSIVELY INTENDED FOR LABORATORY AND RESEARCH USE.

Any clinical research initiatives must be conducted under the guidance of the relevant Institutional Review Board (IRB). Similarly, preclinical research involving animals must comply with the directives of the Institutional Animal Care and Use Committee (IACUC), adhering to the standards delineated by the Animal Welfare Act (AWA).

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IMPORTANT NOTICE: All products showcased on our platform are EXCLUSIVELY INTENDED FOR LABORATORY AND RESEARCH APPLICATIONS. They are expressly not intended for veterinary or human utilization.

References

1. Pavlov VA, Ochani M, Yang LH, Gallowitsch-Puerta M, Ochani K, Lin X, Levi J, Parrish WR, Rosas-Ballina M, Czura CJ, Larosa GJ, Miller EJ, Tracey KJ, Al-Abed Y. Selective alpha7-nicotinic acetylcholine receptor agonist GTS-21 improves survival in murine endotoxemia and severe sepsis. Crit Care Med. 2007 Apr;35(4):1139-44. doi: 10.1097/01.CCM.0000259381.56526.96. PMID: 17334244. Read More
2. Kitagawa H, Takenouchi T, Azuma R, Wesnes KA, Kramer WG, Clody DE, Burnett AL. Safety, pharmacokinetics, and effects on cognitive function of multiple doses of GTS-21 in healthy, male volunteers. Neuropsychopharmacology. 2003 Mar;28(3):542-51. doi: 10.1038/sj.npp.1300028. PMID: 12629535. Read More
3. Kong FJ, Ma LL, Zhang HH, Zhou JQ. Alpha 7 nicotinic acetylcholine receptor agonist GTS-21 mitigates isoflurane-induced cognitive impairment in aged rats. J Surg Res. 2015 Jan;194(1):255-61. doi: 10.1016/j.jss.2014.09.043. PMID: 25450597. Read More