Sazetidine A dihydrochloride
Chemical Name: 6-[5-[(2S)-2-Azetidinylmethoxy]-3-pyridinyl]-5-hexyn-1-ol dihydrochloride
Purity: ≥98%
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
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
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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 -
Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them.
Xiao et al.
Mol.Pharmacol., 2006;70:1454 -
Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug.
Cucchiaro et al.
Anesthesiology, 2008;109:512 -
Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors.
Zwart et al.
Mol.Pharmacol., 2008;73:1843
Product Datasheets
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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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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
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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
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Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors.
Authors: Brown and Wonnacott
PLoS One 2015;40:2047
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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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