| 3-pyr-Cytisineα4β2 receptors agonist |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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| Cas No. | 948027-43-8 | SDF | Download SDF |
| Chemical Name | (1R,5S)-9-(pyridin-3-yl)-3,4,5,6-tetrahydro-1H-1,5-methanopyrido[1,2-a][1,5]diazocin-8(2H)-one | ||
| Canonical SMILES | O=C1C(C2=CN=CC=C2)=CC=C3[C@]4([H])C[C@@](CN31)([H])CNC4 | ||
| Formula | C16H17N3O | M.Wt | 267.33 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | White solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
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.
