• CAS 156223-05-1 Nootropic GTS-21 (DMXB-A) Powder
  • CAS 156223-05-1 Nootropic GTS-21 (DMXB-A) Powder
CAS 156223-05-1 Nootropic GTS-21 (DMXB-A) Powder
  • Wuhan Hengheda Pharm Co.,Ltd
  • China
  • Immediately after payment
  • 10kg/month

GTS-21 (also known as DMBX-A), is a novel, small-molecule, orally active and selective alpha-7 nicotinic acetylcholine (nACh) receptor agonist that has demonstrated memory and cognition enhancement activity in human clinical trials. Athenagen licensed the exclusive rights to the compound and a related library of analogs as part of the acquisition of Osprey Pharmaceutical Company in April 2006. GTS-21 has been studied in multiple Phase I studies in healthy volunteers and one Phase I/II study in schizophrenic patients. In all studies, the compound was well tolerated. In a Phase I multi-dose, double-blind, placebo controlled study in healthy adults, GTS-21 also demonstrated cognitive enhancement across all doses, with a statistically significant improvement in attention related and memory related tasks.
GTS-21 was O-demethylated to yield compounds that were then subject to glucuronidation. Three of the metabolites in rat urine were isolated and characterized as 4-OH-GTS-21, 4-OH-GTS-21 glucuronide and 2-OH-GTS-21 glucuronide. The major urinary metabolites were 4-OH-GTS-21 glucuronide and 2-OH-GTS-21 glucuronide. In vitro chemical inhibition of cytochrome P450 in human liver microsomes indicated that CYPIA2 and CYP2E1 were the isoforms primarily responsible for the O-demethylation of GTS-21, with some contribution from CYP3A.

CAS 156223-05-1 Nootropic GTS-21 (DMXB-A) Powder

Identification of nicotinic receptor subtypes involved in nicotine dependence is required for guiding the design of more selective antagonists capable of blocking the nicotine cue and nicotine self-administration. Due to the multiplicity of nicotinic receptors in the mammalian brain, selective agonists and antagonists are needed to assess the functional involvement of a particular subtype in vivo. Only recently have a few nicotinic receptor subtype-selective antagonists and agonists been identified. GTS-21 (also known as DMBX-anabaseine) is the only agent so far reported that selectively stimulates the alpha7 nicotinic receptor. Here GTS-21 was used to assess the possible mediation of the nicotine cue by this receptor subtype. Long-Evans rats were trained to discriminate between presession administration of 0.10 or 0.40 mg/kg (-)-nicotine bitartrate and its vehicle. GTS-21 did not substitute for nicotine, as all subjects consistently chose the vehicle lever after GTS-21 substitution. In another experiment, different doses of GTS-21 were administered prior to nicotine administration to investigate whether GTS-21 would antagonize the nicotine cue. Such was not the case. The lack of effect of GTS-21 upon the nicotine cue is consistent with the notion that the cue is mediated by nicotinic receptors other than the alpha7 receptor.

Cardiovascular disease, specifically heart failure affects nearly 6 million Americans, and remains to be the number one cause of hospitalization and death globally. Multiple studies have suggested that inflammation plays a pivotal role in the pathogenesis of this disease. There is a novel link between the vagus nerve and the inflammatory responses, where the vagus nerve can limit inflammation via the alpha-7 nicotinic acetylcholine receptor (α7 nAChR) in relation to the “cholinergic anti-inflammatory pathway (CAP)”. Selective pharmacological stimulation of the α7 nAChR may have therapeutic potential for the treatment of inflammatory conditions. We determined the anti-inflammatory potential of 3-(2,4-dimethoxybenzylident)-anabaseine (GTS-21), an α7-selective partial agonist, in an in vivo zebrafish heart failure model. To investigate the possible therapeutic benefit of GTS- 21, we used a chronic exposure system in which animals are pre-treated with GTS-21 for 20 minutes per day for four consecutive days. On day four after a short washout period, heart failure is chemically induced by Oligo-[2-(2- ethoxy)-ethoxyethyl)-guanidinium-chloride] (PGH) and survival is recorded. We show that GTS-21 has a profound anti-inflammatory effect in improving survivability in a concentration dependent manner. Moreover, rtPCR analysis on heart tissue shows that pre-treatment with GTS-21 induces modifications in levels of gene regulatory proteins leading to altered cytokine expression within the myocardium. In all, these data indicate that GTS-21 may be a promising therapeutic as it influences the inflammatory response in heart failure.

Do we have the test reports for our products provided by the independent third party?
Every batch of our product was tested by authorized independent third party, Analysis testing center, Shanghai branch, Chinese Academy of Science. We send goods to customers with test report and COA. Our products were also tested by American Analytical Chemistry Laboratories and Chromadex too....more
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