Sazetidine A dihydrochloride
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.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 333.25. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3 mL||15 mL||30.01 mL|
|5 mM||0.6 mL||3 mL||6 mL|
|10 mM||0.3 mL||1.5 mL||3 mL|
|50 mM||0.06 mL||0.3 mL||0.6 mL|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
References are publications that support the products' biological activity.
Xiao et al (2006) Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them. Mol.Pharmacol. 70 1454 PMID: 16857741
Cucchiaro et al (2008) Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug. Anesthesiology 109 512 PMID: 18719450
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
If you know of a relevant reference for Sazetidine A dihydrochloride, please let us know.
Keywords: α4β2 a4b2 receptor ligands agonists desensitizers desensitisers Nicotinic Receptors Acetylcholine nAChR SazetidineA dihydrochloride Nicotinic (a4b2) Receptors
2 Citations for Sazetidine A dihydrochloride
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
Do you know of a great paper that uses Sazetidine A dihydrochloride from Tocris? If so please let us know.
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