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GTS 21 dihydrochloride nAChRs agonist, novel

Catalog No.B7682
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Chemical structure

GTS 21 dihydrochloride

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Chemical Properties

Cas No. 156223-05-1 SDF Download SDF
Chemical Name (E)-3-(2,4-dimethoxybenzylidene)-3,4,5,6-tetrahydro-2,3'-bipyridine dihydrochloride
Canonical SMILES COC1=CC(OC)=C(/C([H])=C2CCCN=C\2C3=CN=CC=C3)C=C1.Cl.Cl
Formula C19H20N2O2.2HCl M.Wt 381.3
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
Physical Appearance Yellow solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.


GTS 21 dihydrochloride is a novel agonist of nicotinic acetylcholine receptors (nAChRs) [1].
nAChRs are neuron receptor proteins that activated by the binding of the neurotransmitter acetylcholine (ACh).  
In RAW 264.7 cells (a macrophage like cell line) exposed to hyperoxia (≥99% O2), GTS-21 significantly increased phagocytic activity of macrophages in a dose-dependent way and reduced hyperoxia-induced hyperacetylation of HMGB1. Also, GTS-21 inhibited the cytoplasmic translocation and release of HMGB1 from these macrophages [1]. GTS-21 bound to human α4β2 nAChR (Ki value of 20 nM) 100-fold more potently than to human α7 nAChR, and was 2- and 18-fold less potent than (2)-nicotine at human α7 and α4β2 nAChR, respectively [2].    
In mice that were exposed to hyperoxia (≥99% O2) and subsequently challenged with PA, intraperitoneal injection of GTS-21 (4 mg/kg) significantly increased bacterial clearance, decreased accumulation of airway HMGB1 and decreased acute lung injury [1]. GTS-21 stimulated dopamine release from rat striatal slices with an EC50 of 10uM. In the delayed matching-to-sample task, GTS-21 (32–130 nmol/kg) improved learning performance of monkeys [2].
[1]. Sitapara RA, Antoine DJ, Sharma L, et al. The α7 nicotinic acetylcholine receptor agonist GTS-21 improves bacterial clearance in mice by restoring hyperoxia-compromised macrophage function. Mol Med, 2014, 20: 238-247.
[2]. Briggs CA, Anderson DJ, Brioni JD, et al. Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo. Pharmacol Biochem Behav, 1997, 57(1-2): 231-241.