Sazetidine A dihydrochloride
Chemical Name: 6-[5-[(2S)-2-Azetidinylmethoxy]-3-pyridinyl]-5-hexyn-1-ol dihydrochloride
Biological ActivitySazetidine 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Sazetidine-A, a selective α4β2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats.
Levin et al.
Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them.
Xiao et al.
Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug.
Cucchiaro et al.
Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors.
Zwart et al.
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
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
Inhibition of peripheral macrophages by nicotinic acetylcholine receptor agonists suppresses spinal microglial activation and neuropathic pain in mice with peripheral nerve injury.
J Neuroinflammation 2018;15(1):96
Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors.
Authors: Brown and Wonnacott
PLoS One 2015;40:2047
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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