Sazetidine A dihydrochloride
Cat. No. 2736
Chemical Name: 6-[5-[(2S)-2-Azetidinylmethoxy]-3-p
Biological ActivitySubtype-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.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Levin et al (2010) Sazetidine-A, a selective α4β2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats. J.Pharmacol.Exp.Ther. 332 933. PMID: 20007754.
Cucchiaro et al (2008) Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug. Anesthesiology 109 512. PMID: 18719450.
Zwart et al (2008) Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors. Mol.Pharmacol. 73 1843.
Xiao et al (2006) Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them. Mol.Pharmacol. 70 1454. PMID: 16857741.
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Citations are publications that use Tocris products. Selected citations for Sazetidine A dihydrochloride include:
Brown and Wonnacott (2015) Sazetidine-A Activates and Desensitizes Native α7 Nicotinic Acetylcholine Receptors. PLoS One 40 2047. PMID: 24728867.
Kuryatov et al (2013) Chemical chaperones exceed the chaperone effects of RIC-3 in promoting assembly of functional α7 AChRs. Nat Commun 8 e62246. PMID: 23638015.
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