Partial agonist at α7nACh receptors. Binds selectively to α7 subunits, with no significant activity seen at α2, α3 and α4. (EC50 = 10 μM in vitro (striatal slices)). Shown to elicit nootropic, neuroprotective and anti-inflammatory effects.
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Soluble in water to 100 mM and in DMSO to 100 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Kox M et al. a7 nicotinic acetylcholine receptor agonist GTS-21 attenuates ventilator-induced tumour necrosis factor-a production and lung injury. Br J Anaesth107:559-66 (2011).
Read more (PubMed: 21771746) »
Stevens KE et al. Continuous administration of a selective alpha7 nicotinic partial agonist, DMXBA, improves sensory inhibition without causing tachyphylaxis or receptor upregulation in DBA/2 mice. Brain Res1352:140-6 (2010).
Read more (PubMed: 20599427) »
Meyer EM et al. 3-[2,4-Dimethoxybenzylidene]anabaseine (DMXB) selectively activates rat alpha7 receptors and improves memory-related behaviors in a mecamylamine-sensitive manner. Brain Res768:49-56 (1997).
Read more (PubMed: 9369300) »
Rosas-Ballina M et al. The selective alpha7 agonist GTS-21 attenuates cytokine production in human whole blood and human monocytes activated by ligands for TLR2, TLR3, TLR4, TLR9, and RAGE. Mol Med15:195-202 (0).
Read more (PubMed: 19593403) »
Briggs CA et al. Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo. Pharmacol Biochem Behav57:231-41 (0).
Read more (PubMed: 9164577) »