Sazetidine A dihydrochloride

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Sazetidine A dihydrochloride | Additional Nicotinic (a4b2) Receptor Compounds
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Description: α4β2 nAChR ligand; may act as an agonist or a desensitizer

Chemical Name: 6-[5-[(2S)-2-Azetidinylmethoxy]-3-pyridinyl]-5-hexyn-1-ol dihydrochloride

Purity: ≥98%

Product Details
Citations (4)
Supplemental Products

Biological Activity

Sazetidine A dihydrochloride is a 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

Soluble to 50 mM in water
Desiccate at +4°C

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. 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
  2. Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them.
    Xiao et al.
    Mol.Pharmacol., 2006;70:1454
  3. Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug.
    Cucchiaro et al.
    Anesthesiology, 2008;109:512
  4. Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors.
    Zwart et al.
    Mol.Pharmacol., 2008;73:1843

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Citations for Sazetidine A dihydrochloride

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

4 Citations: Showing 1 - 4


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