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Sazetidine A dihydrochloride

CAS# 1197329-42-2

Sazetidine A dihydrochloride

Catalog No. BCC7468----Order now to get a substantial discount!

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Chemical structure

Sazetidine A dihydrochloride

3D structure

Chemical Properties of Sazetidine A dihydrochloride

Cas No. 1197329-42-2 SDF Download SDF
PubChem ID 56972183 Appearance Powder
Formula C15H22Cl2N2O2 M.Wt 333.25
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in water
Chemical Name 6-[5-[[(2S)-azetidin-2-yl]methoxy]pyridin-3-yl]hex-5-yn-1-ol;dihydrochloride
SMILES C1CNC1COC2=CN=CC(=C2)C#CCCCCO.Cl.Cl
Standard InChIKey WRSKKJWUXISFFU-UTLKBRERSA-N
Standard InChI InChI=1S/C15H20N2O2.2ClH/c18-8-4-2-1-3-5-13-9-15(11-16-10-13)19-12-14-6-7-17-14;;/h9-11,14,17-18H,1-2,4,6-8,12H2;2*1H/t14-;;/m0../s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Sazetidine A dihydrochloride

DescriptionSubtype-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.

Sazetidine A dihydrochloride Dilution Calculator

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Preparing Stock Solutions of Sazetidine A dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.0008 mL 15.0038 mL 30.0075 mL 60.015 mL 75.0188 mL
5 mM 0.6002 mL 3.0008 mL 6.0015 mL 12.003 mL 15.0038 mL
10 mM 0.3001 mL 1.5004 mL 3.0008 mL 6.0015 mL 7.5019 mL
50 mM 0.06 mL 0.3001 mL 0.6002 mL 1.2003 mL 1.5004 mL
100 mM 0.03 mL 0.15 mL 0.3001 mL 0.6002 mL 0.7502 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Sazetidine A dihydrochloride

Sazetidine-A, a selective alpha4beta2 nicotinic receptor desensitizing agent and partial agonist, reduces nicotine self-administration in rats.[Pubmed:20007754]

J Pharmacol Exp Ther. 2010 Mar;332(3):933-9.

Adequate treatment of tobacco addiction remains problematic. Part of the problem with treatment is a poor understanding of the pharmacologic aspects of nicotine contributing to addiction. In addition to activating nicotinic acetylcholine receptors, nicotine also desensitizes them. It is currently not known how much of each of nicotine's actions contribute to its particular behavioral effects. Sazetidine-A (saz-A) is a novel nicotinic receptor-desensitizing agent and partial agonist with high selectivity for alpha4beta2 receptors. The current experiments were conducted to determine whether saz-A would reduce nicotine self-administration in rats and to characterize its ancillary effects. Adult male Sprague-Dawley rats were allowed to self-administer nicotine. After initial food pellet training followed by 10 sessions of nicotine self-administration training, the rats were administered saz-A (0.1-3 mg/kg s.c.) or the saline vehicle in a repeated-measures counterbalanced design. Saz-A at the 3 mg/kg dose significantly decreased nicotine self-administration relative to performance of the same rats after saline injections. In a second study, long-term administration of this dose of sazetidine-A over the course of 10 sessions significantly reduced nicotine self-administration with no apparent diminution of effect. Saz-A in this dose range had only modest effects on locomotor activity, without any overall decrease in activity over a 1-h-long session. Saz-A significantly reduced food self-administration, but this effect was smaller than its effect on nicotine self-administration. Saz-A, which is a selective alpha4beta2-desensitizing agent and partial agonist, effectively reduces nicotine self-administration. This type of treatment holds promise for a new therapy to aid smoking cessation.

Analgesic effects of Sazetidine-A, a new nicotinic cholinergic drug.[Pubmed:18719450]

Anesthesiology. 2008 Sep;109(3):512-9.

BACKGROUND: The use of nicotinic agonists for analgesia is limited by their unacceptable side effects. Sazetidine-A is a new partial agonist nicotinic ligand that has very high selectivity for beta2-containing nicotinic acetylcholine receptors. It potently and selectively desensitizes alpha4beta2 nicotinic acetylcholine receptors without measurable effects on alpha3beta4 receptors. The authors investigated the analgesic effects of Sazetidine-A using the formalin model of chronic inflammatory pain. METHODS: The formalin test was conducted after rats received intraperitoneal saline, Sazetidine-A (0.125, 0.25, 0.5, 1, 2 mg/kg), or subcutaneous epibatidine (2.5-5-10 mug/kg). In other experiments, Sazetidine-A was preceded by naloxone (0.5 mg/kg) or mecamylamine (10 mg). Effects of Sazetidine-A and epibatidine on locomotor were tested in an open field, and seizure activity was measured using the Racine scale. Locus coeruleus neuron extracellular single-unit spontaneous discharge was recorded in anesthetized animals after Sazetidine-A and epibatidine. RESULTS: Higher doses of Sazetidine-A (0.5, 1, or 2 mg/kg) induced analgesia, with pain scores significantly lower than those seen after saline, lower doses of Sazetidine-A, and epibatidine (P < 0.001). Naloxone did not antagonize the effects of Sazetidine-A, and mecamylamine had partial, dose-dependent antagonistic effects. Epibatidine excited locus coeruleus neurons, whereas Sazetidine-A had no effect on these neurons. Epibatidine and Sazetidine-A affected animals' locomotor activity for the initial 20 min. While analgesic doses of epibatidine caused seizures, no seizure activity or other neurologic complications were seen in animals that received as much as four times the minimum analgesic dose of Sazetidine-A. CONCLUSIONS: Sazetidine-A seems to be a potent analgesic without causing neurologic side effects.

Sazetidine-A, a novel ligand that desensitizes alpha4beta2 nicotinic acetylcholine receptors without activating them.[Pubmed:16857741]

Mol Pharmacol. 2006 Oct;70(4):1454-60.

Neuronal nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels found throughout the central and peripheral nervous systems. They are crucial to normal physiology and have been clearly implicated in nicotine addiction. In addition, they are possible therapeutic targets in a wide range of pathological conditions, including cognitive disorders, Parkinson's disease, and neuropathic pain. Nicotinic ligands are usually classified as agonists (or partial agonists), competitive antagonists, or noncompetitive antagonists. Sazetidine-A is a new nicotinic ligand that shows a different pharmacological profile from any of these known classes of ligands. Sazetidine-A competes with very high binding affinity (Ki approximately 0.5 nM) and selectivity for the alpha4beta2 nAChR subtype (Ki ratio alpha3beta4/alpha4beta2 approximately 24,000). Despite its high affinity, sazetidine-A neither activates nAChR channel function nor prevents channel activation when it is applied simultaneously with nicotine. However, when it is pre-incubated for 10 min with the receptors, it potently blocks nicotine-stimulated alpha4beta2 nAChR function (IC50 approximately 30 nM). The action of sazetidine-A may be explained by its very low affinity for the resting conformation of the alpha4beta2 nAChRs, and its very high affinity for the desensitized state of the receptor. We propose that sazetidine-A is a "silent desensitizer" of nAChRs, meaning that it desensitizes the receptor without first activating it. Furthermore, comparison of the effects of sazetidine-A and nicotine at alpha4beta2 nAChRs suggests that the predominant effects of nicotine and other nicotinic agonists are related to desensitization of the receptors and that sazetidine-A potently mimics these effects.

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