GTS 21 dihydrochloride

Biological Activity

GTS 21 dihydrochloride is a partial agonist of α7 nicotinic acetylcholine receptors (nAChRs); also a weak α4β2 and 5-HT₃ antagonist at micromolar concentrations. Exhibits improved sensory inhibition in DBA/2 mice following both acute and chronic administration. Also shown to improve memory in several animal models; facilitates hippocampal long-term potentiation. Also has anti-inflammatory effects independent of α7 nAChRs.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Continuous administration of a selective alpha7 nicotinic partial agonist, DMXBA, improves sensory inhibition without causing tachyphylaxis or receptor upregulation in DBA/2 mice.
   Stevens et al.
   Brain.Res., 2010;1352:140
2. Effects of anabaseine-related analogs on rat brain nicotinic receptor binding and on avoidance behaviors.
   Meyer et al.
   Drug Dev.Res., 1994;31:127
3. Nicotinic mechanisms in the treatment of psychotic disorders: a focus on the a7 nicotinic receptor.
   Olincy et al.
   Handb.Exp.Pharmacol., 2012;213:211
4. GTS-21 has cell-specific anti-inflammatory effects independent of a7 nicotinic acetylcholine receptors.
   Garg and Loring et al.
   PLoS One, 2019;14:e0214942

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