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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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||6 mL||30.01 mL||60.02 mL|
|2.5 mM||1.2 mL||6 mL||12 mL|
|5 mM||0.6 mL||3 mL||6 mL|
|25 mM||0.12 mL||0.6 mL||1.2 mL|
References are publications that support the biological activity of the product.
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
Zwart et al (2008) Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors. Mol.Pharmacol. 73 1843
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Keywords: Sazetidine A dihydrochloride, Sazetidine A dihydrochloride supplier, α4β2, a4b2, receptor, ligands, agonists, desensitizers, desensitisers, Nicotinic, Receptors, Acetylcholine, nAChR, SazetidineA, dihydrochloride, 1197329-42-2, (a4b2), 2736, Tocris Bioscience
4 Citations for Sazetidine A dihydrochloride
Citations are publications that use Tocris products. Selected citations for Sazetidine A dihydrochloride include:
Kutlu et al (2018) Differential effects of α4β2 nicotinic receptor antagonists and partial-agonists on contextual fear extinction in male C57BL/6 mice. Psychopharmacology (Berl) 235 1211 PMID: 29383396
Kiguchi (2018) Inhibition of peripheral macrophages by nicotinic acetylcholine receptor agonists suppresses spinal microglial activation and neuropathic pain in mice with peripheral nerve injury. J Neuroinflammation 15 96 PMID: 29587798
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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.