3-pyr-Cytisine

α4β2 receptors agonist CAS# 948027-43-8

3-pyr-Cytisine

Catalog No. BCC6118----Order now to get a substantial discount!

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Chemical structure

3-pyr-Cytisine

3D structure

Chemical Properties of 3-pyr-Cytisine

Cas No. 948027-43-8 SDF Download SDF
PubChem ID 16731778 Appearance Powder
Formula C16H17N3O M.Wt 267.33
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 100 mM in DMSO
SMILES C1C2CNCC1C3=CC=C(C(=O)N3C2)C4=CN=CC=C4
Standard InChIKey GOYASQWDLRLAPK-WCQYABFASA-N
Standard InChI InChI=1S/C16H17N3O/c20-16-14(12-2-1-5-17-8-12)3-4-15-13-6-11(7-18-9-13)10-19(15)16/h1-5,8,11,13,18H,6-7,9-10H2/t11-,13+/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 3-pyr-Cytisine

DescriptionHigh affinity α4β2 partial agonist (Ki values are 0.91, 119 and 1100 nM for α4β2, α3β4 and α7 receptors respectively). Shows little activity at α3β4 and α7 receptors. Exhibits antidepressant-like effects in mouse models of antidepressant efficacy.

3-pyr-Cytisine Dilution Calculator

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Preparing Stock Solutions of 3-pyr-Cytisine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.7407 mL 18.7035 mL 37.407 mL 74.8139 mL 93.5174 mL
5 mM 0.7481 mL 3.7407 mL 7.4814 mL 14.9628 mL 18.7035 mL
10 mM 0.3741 mL 1.8703 mL 3.7407 mL 7.4814 mL 9.3517 mL
50 mM 0.0748 mL 0.3741 mL 0.7481 mL 1.4963 mL 1.8703 mL
100 mM 0.0374 mL 0.187 mL 0.3741 mL 0.7481 mL 0.9352 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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Background on 3-pyr-Cytisine

3-pyr-Cytisine is a partial agonist of α4β2 receptor with Ki values of 0.91, 119 and 1100 nM for α4β2, α3β4 and α7 receptors, respectively [1].

The alpha-4 beta-2 nicotinic receptor (α4β2 receptor) is a nicotinic acetylcholine receptor participated in learning and is widely expressed in the central nervous system. Also, α4β2 receptor has the highest affinity for nicotine.

3-pyr-Cytisine is an α4β2 receptor partial agonist. In cells expressed α4β2 receptor, 3-pyr-Cyt reduced the agonist response by ACh, which relayed on the intrinsic activity of 3-pyr-Cyt and 3-pyr-Cyt concentration [1]. In PC12 cells, 3-pyr-Cyt significantly induced release of norepinephrine (NE) in a time-, dose- and Ca2+-dependent way. Also, 3-pyr-Cyt inhibited nicotine-induced NE release and increased the mRNA levels of tyrosine hydroxylase (TH), which is necessary for catecholamine biosynthetic [2].

In the tail suspension test, mice treated with 3-pyr-Cyt (0.6 mg/kg) spent significantly less time immobile in a dose-dependent way. In the forced swim test, mice treated with 3-pyr-Cyt (0.3, 0.6 or 0.9 mg/kg) were significantly less immobile in a dose-dependent way, which suggested that 3-pyr-Cyt exhibited antidepressant-like effects in a dose-dependent way [1].

References:
[1].  Mineur YS, Eibl C, Young G, et al. Cytisine-based nicotinic partial agonists as novel antidepressant compounds. J Pharmacol Exp Ther, 2009, 329(1): 377-386.
[2].  Turcanu DS, Kirtok N, Eibl C, et al. Nicotinic receptor partial agonists alter catecholamine homeostasis and response to nicotine in PC12 cells. Neurosci Lett, 2012, 516(2): 212-216.

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References on 3-pyr-Cytisine

Cytisine-based nicotinic partial agonists as novel antidepressant compounds.[Pubmed:19164465]

J Pharmacol Exp Ther. 2009 Apr;329(1):377-86.

Nicotine and other nicotinic agents are thought to regulate mood in human subjects and have antidepressant-like properties in animal models. Recent studies have demonstrated that blockade of nicotinic acetylcholine receptors (nAChRs) including those containing the beta2 subunit (beta2(*)), results in antidepressant-like effects. Previous studies have shown that cytisine, a partial agonist at alpha4/beta2(*) nAChRs, and a full agonist at alpha3/beta4(*) and alpha7 nAChRs, has antidepressant-like properties in several rodent models of antidepressant efficacy; however, it is not clear whether more selective partial agonists will also be effective in these models. We tested cytisine and two derivatives, 5-bromo-cytisine (5-Br-Cyt) and 3-(pyridin-3'-yl)-cytisine (3-pyr-Cyt) for their ability to act as a partial agonist of different nAChR subtypes and to show antidepressant-like activity in C57/BL6 mice in the tail suspension, the forced-swim, and the novelty-suppressed feeding tests. 3-pyr-Cyt was a partial agonist with very low efficacy at alpha4/beta2(*) nAChRS but had no agonist effects at other nAChRs normally targeted by cytisine, and it was effective in mouse models of antidepressant efficacy. Animals showed dose-dependent antidepressant-like effects in all three behavioral paradigms. 5-Br-Cyt was not effective in behavioral tests when administered peripherally, probably because of its inability to penetrate the blood-brain barrier, because it efficiently reduced immobility in the tail suspension test when administered intraventricularly. These results suggest that novel nicotinic partial agonists may provide new possibilities for development of drugs to treat mood disorders.

Activation and inhibition of mouse muscle and neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes.[Pubmed:20100906]

J Pharmacol Exp Ther. 2010 May;333(2):501-18.

Transgenic mouse models with nicotinic acetylcholine receptor (nAChR) knockouts and knockins have provided important insights into the molecular substrates of addiction and disease. However, most studies of heterologously expressed neuronal nAChR have used clones obtained from other species, usually human or rat. In this work, we use mouse clones expressed in Xenopus oocytes to provide a relatively comprehensive characterization of the three primary classes of nAChR: muscle-type receptors, heteromeric neuronal receptors, and homomeric alpha7-type receptors. We evaluated the activation of these receptor subtypes with acetylcholine and cytisine-related compounds, including varenicline. We also characterized the activity of classic nAChR antagonists, confirming the utility of mecamylamine and dihydro-beta-erythroidine as selective antagonists in mouse models of alpha3beta4 and alpha4beta2 receptors, respectively. We also conducted an in-depth analysis of decamethonium and hexamethonium on muscle and neuronal receptor subtypes. Our data indicate that, as with receptors cloned from other species, pairwise expression of neuronal alpha and beta subunits in oocytes generates heterogeneous populations of receptors, most likely caused by variations in subunit stoichiometry. Coexpression of the mouse alpha5 subunit had varying effects, depending on the other subunits expressed. The properties of cytisine-related compounds are similar for mouse, rat, and human nAChR, except that varenicline produced greater residual inhibition of mouse alpha4beta2 receptors than with human receptors. We confirm that decamethonium is a partial agonist, selective for muscle-type receptors, but also note that it is a nondepolarizing antagonist for neuronal-type receptors. Hexamethonium was a relatively nonselective antagonist with mixed competitive and noncompetitive activity.

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