Sazetidine A dihydrochloride

Product Description

Sazetidine A dihydrochloride is a subtype-selective α4β2 nicotinic acetylcholine receptor ligand (K_i 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.

Solubility

Preparing Stock Solutions for Sazetidine A dihydrochloride

The following data is based on the product molecular weight 333.25

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.5 mM	6.00 mL	30.01 mL	60.02 mL
2.5 mM	1.20 mL	6.00 mL	12.00 mL
5 mM	0.60 mL	3.00 mL	6.00 mL
25 mM	0.12 mL	0.60 mL	1.20 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Zwart Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors. Mol.Pharmacol.
• Cucchiaro Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug. Anesthesiology 2008 PMID: 18719450
• Levin Sazetidine-A, a selective α4β2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats. J.Pharmacol.Exp.Ther. 2010 PMID: 20007754
• Xiao Sazetidine-A, a novel ligand that desensitizes α4β2 nicotinic acetylcholine receptors without activating them. Mol.Pharmacol. 2006 PMID: 16857741