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Sazetidine A dihydrochloride

Catalog #: 2736
4 Citations Datasheet / COA / SDS
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2736/10
Sazetidine A dihydrochloride | CAS No. 2455450-63-0 | 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)
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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

M.Wt:
333.25
Formula:
C15H20N2O2.2HCl
Solubility:
Soluble to 50 mM in water
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2455450-63-0

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
  5. Nicotinic acetylcholine receptors: Ex-vivo expression of functional, non-hybrid, heteropentameric receptors from a marine arthropod, Lepeophtheirus salmonis
    L Rufener, K Kaur, A Sarr, SM Aaen, TE Horsberg
    PLoS Pathog., 2020;16(7):e1008715.

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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

  1. Differential effects of α4β2 nicotinic receptor antagonists and partial-agonists on contextual fear extinction in male C57BL/6 mice.
    Authors: Kutlu Et al.
    Psychopharmacology (Berl)  2018;235:1211
  2. Inhibition of peripheral macrophages by nicotinic acetylcholine receptor agonists suppresses spinal microglial activation and neuropathic pain in mice with peripheral nerve injury.
    Authors: Kiguchi
    J Neuroinflammation  2018;15(1):96
  3. Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors.
    Authors: Brown and Wonnacott
    PLoS One  2015;40:2047
  4. Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs.
    Authors: Kuryatov Et al.
    Nat Commun  2013;8:e62246

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