An agonist of α7-containing nAChRs
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GTS-21 (hydrochloride)

Item No. 21570

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3E)-3-[(2,4-dimethoxyphenyl)methylene]-3,4,5,6-tetrahydro-2,3'-bipyridine, dihydrochloride
CAS Number
156223-05-1
Synonyms
  • DMXB-A
Molecular Formula
C19H20N2O2 • 2HCl
Formula Weight
381.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 2 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
258, 406 nm
SMILES
COC1=C(/C=C2CCCN=C\2C3=CN=CC=C3)C=CC(OC)=C1.Cl.Cl
InChi Code
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+;;
InChi Key
BXKYFUGAAFLYJL-BXGYHSFXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    25 mg

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    50 mg

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    Product Description

    GTS-21 is an agonist of α7-containing nicotinic acetylcholine receptors (nAChRs) that, at a concentration of 100 μM, activates human α7-containing nAChRs expressed in Xenopus oocytes to 60% of the levels generated by endogenous ligand acetylcholine.1 It is selective for α7-containing nAChRs, having no activity at α2-, α3-, and α4-containing nAChRs at a concentration of 100 μM. GTS-21 stimulates dopamine release from rat striatal slices (EC50 = 10 μM).2 In vivo, GTS-21 decreases delay in the delayed matching-to-sample task in monkeys. It also suppresses amnesia and neuronal cell death in a gerbil model of ischemia-reperfusion injury.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Meyer, E.M., Tay, E.T., Papke, R.L., et al. 3-[2,4-Dimethoxybenzylidene]anabaseine (DMXB) selectively activates rat α7 receptors and improves memory-related behaviors in a mecamylamine-sensitive manner. Brain Res. 768(1-2), 49-56 (1997).

    2. Briggs, C.A., Anderson, D.J., Brioni, J.D., et al. Functional characterization of the novel neuronal nicotinic acetylcholine receptor ligand GTS-21 in vitro and in vivo. Pharmacol. Biochem. Behav. 57(1-2), 231-241 (1997).

    3. Nanri, M., Yamamoto, J., Miyake, H., et al. Protective effect of GTS-21, a novel nicotinic receptor agonist, on delayed neuronal death induced by ischemia in gerbils. Jpn. J. Pharmacol. 76(1), 23-29 (1998).