Catalog Number: 2736
Chemical Name: 6-[5-[(2S)-2-Azetidinylmethoxy]-3-pyridinyl]-5-hexyn-1-ol dihydrochloride
Biological Activity
Subtype-selective α4β2 nicotinic acetylcholine receptor ligand (Ki values are 0.26 and 54 nM at α4β2 and α3β4 receptors respectively). May act as a silent desensitizer or as an agonist, depending on subunit stoichiometry (EC50 = 1.1 nM for nAChR-stimulated dopamine release). Exhibits analgesic activity in vivo and significantly reduces nicotine self-administration in an experimental rat model.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in water
  • Purity:
  • Storage:
    Desiccate at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them.
    Xiao et al.
    Mol.Pharmacol., 2006;70:1454
  2. Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug.
    Cucchiaro et al.
    Anesthesiology, 2008;109:512
  3. Sazetidine-A, a selective α4β2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats.
    Levin et al.
    J.Pharmacol.Exp.Ther., 2010;332:933
  4. Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors.
    Zwart et al.
    Mol.Pharmacol., 2008;73:1843

The citations listed below are publications that use Tocris products. Selected citations for Sazetidine A dihydrochloride include:

Showing Results 1 - 2 of 2

  1. Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors.
    Authors: Brown and Wonnacott
    PLoS One
  2. Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs.
    Authors: Kuryatov Et al.
    Nat Commun
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