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 / Safety Data Sheet
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.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products.
Do you know of a great paper that uses Sazetidine A dihydrochloride from Tocris? If so please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: Sazetidine A dihydrochloride, supplier, α4β2, a4b2, receptor, ligands, agonists, desensitizers, desensitisers, Nicotinic, Receptors, Acetylcholine, nAChR, SazetidineA, dihydrochloride, Tocris Bioscience, Nicotinic (α4β2) Receptor products