For research use only. Not for therapeutic Use.
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist[1][2].
GTS-21 bound to human α4β2 nAChR (Ki=20 nM) 100-fold more potently than to humanα7-nAChR, and is 18- and 2-fold less potent than (-)-nicotine at human α4β2 and a7 nAChR, respectively[1].
GTS 21 (4 mg/kg; i.p.; 1, 3, 7, 14 and 21 days) reduces radiation induced histological signs of pulmonary injury[3].
| Catalog Number | I001982 |
| CAS Number | 156223-05-1 |
| Synonyms | 3-[(5E)-5-[(2,4-dimethoxyphenyl)methylidene]-3,4-dihydro-2H-pyridin-6-yl]pyridine;dihydrochloride |
| Molecular Formula | C19H22Cl2N2O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H20N2O2.2ClH/c1-22-17-8-7-14(18(12-17)23-2)11-15-5-4-10-21-19(15)16-6-3-9-20-13-16;;/h3,6-9,11-13H,4-5,10H2,1-2H3;2*1H/b15-11+;; |
| InChIKey | BXKYFUGAAFLYJL-BXGYHSFXSA-N |
| SMILES | COC1=CC(=C(C=C1)C=C2CCCN=C2C3=CN=CC=C3)OC.Cl.Cl |
| Reference | [1]. Briggs CA, 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. [2]. Zhang R, et al. N-terminal domains in mouse and human 5-hydroxytryptamine3A receptors confer partial agonist and antagonist properties to benzylidene analogs of anabaseine. J Pharmacol Exp Ther. 2006;317(3):1276-1284. [3]. Mei Z, et al. α7 nAchR agonist GTS 21 reduces radiation induced lung injury. Oncol Rep. 2018;40(4):2287-2297. |
