Sazetidine A dihydrochloride

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Cat.No. 2736 - Sazetidine A dihydrochloride | C15H20N2O2.2HCl | CAS No. 1197329-42-2
Description: α4β2 receptor ligand; may act as an agonist or a desensitizer
Chemical Name: 6-[5-[(2S)-2-Azetidinylmethoxy]-3-pyridinyl]-5-hexyn-1-ol dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Literature

Biological Activity

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.

Technical Data

M. Wt 333.25
Formula C15H20N2O2.2HCl
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 1197329-42-2
PubChem ID 56972183
InChI Key WRSKKJWUXISFFU-UTLKBRERSA-N
Smiles OCCCCC#CC1=CN=CC(OC[C@H]2NCC2)=C1.Cl.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 16.66 50

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.

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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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

Zwart et al (2008) Sazetidine-A is a potent and selective agonist at native recombinant α4β2 nicotinic acetylcholine receptors. Mol.Pharmacol. 73 1843 PMID:


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


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