UB 165 fumarateSubunit selective nAChR agonist CAS# 200432-86-6 |
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Quality Control & MSDS
3D structure
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| Cas No. | 200432-86-6 | SDF | Download SDF |
| PubChem ID | 71297058 | Appearance | Powder |
| Formula | C17H19ClN2O4 | M.Wt | 350.8 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in water with gentle warming | ||
| Chemical Name | (E)-but-2-enedioic acid;2-(6-chloropyridin-3-yl)-9-azabicyclo[4.2.1]non-2-ene | ||
| SMILES | C1CC2CCC(N2)C(=C1)C3=CN=C(C=C3)Cl.C(=CC(=O)O)C(=O)O | ||
| Standard InChIKey | DZFRKSLRKAKJIB-WLHGVMLRSA-N | ||
| Standard InChI | InChI=1S/C13H15ClN2.C4H4O4/c14-13-7-4-9(8-15-13)11-3-1-2-10-5-6-12(11)16-10;5-3(6)1-2-4(7)8/h3-4,7-8,10,12,16H,1-2,5-6H2;1-2H,(H,5,6)(H,7,8)/b;2-1+ | ||
| 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. |
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| 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. |
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| 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. | ||
| Description | Subtype-selective nicotinic agonist. Full agonist at α3β2- and very weak partial agonist at α4β2- containing nAChRs. Ki values are 0.27, 20 (IC50), 2790 and 990 nM for α4β2, α3, α7 and α1β1δε respectively. |
UB 165 fumarate Dilution Calculator
UB 165 fumarate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.8506 mL | 14.2531 mL | 28.5063 mL | 57.0125 mL | 71.2657 mL |
| 5 mM | 0.5701 mL | 2.8506 mL | 5.7013 mL | 11.4025 mL | 14.2531 mL |
| 10 mM | 0.2851 mL | 1.4253 mL | 2.8506 mL | 5.7013 mL | 7.1266 mL |
| 50 mM | 0.057 mL | 0.2851 mL | 0.5701 mL | 1.1403 mL | 1.4253 mL |
| 100 mM | 0.0285 mL | 0.1425 mL | 0.2851 mL | 0.5701 mL | 0.7127 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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Different nicotinic acetylcholine receptor subtypes mediating striatal and prefrontal cortical [3H]dopamine release.[Pubmed:15617729]
Neuropharmacology. 2005 Jan;48(1):72-9.
Different nicotinic acetylcholine receptor subtypes appear to modulate dopamine release from the striatum and prefrontal cortex. In this study a combination of subtype-selective antagonists and agonists were used to extensively characterize the nAChRs involved in dopamine release from slice preparations of these two brain regions. alpha-conotoxin-MII inhibited nicotine-evoked [3H]dopamine (DA) release from striatum by 45%, but did not affect cortical dopamine release. Neither methyllycaconitine, alpha-bungarotoxin, nor alpha-conotoxin-ImI affected nicotine-evoked [3H]DA release from either striatum or prefrontal cortex. MG 624, a novel selective nAChR antagonist, inhibited cortical [3H]DA by 53%, but had no effect on striatal release. Compared to nicotine, (+/-)-UB-165 showed less efficacy with respect to dopamine release from striatum, and had no effect on cortical dopamine release. (+/-)-UB-165-evoked striatal dopamine release was completely blocked by mecamylamine, partially blocked (up to 55%) by alpha-conotoxin-MII, and unaffected by methyllycaconitine or alpha-conotoxin-ImI. alpha4beta2* and alpha6beta2beta3* nAChRs appear to play a role in striatal dopamine release, whereas alpha4beta2* nAChRs modulate release from prefrontal cortex. alpha7* nAChRs do not appear to play a role in nAChR-mediated dopamine release from either brain region.
UB-165: a novel nicotinic agonist with subtype selectivity implicates the alpha4beta2* subtype in the modulation of dopamine release from rat striatal synaptosomes.[Pubmed:10751429]
J Neurosci. 2000 Apr 15;20(8):2783-91.
Presynaptic nicotinic acetylcholine receptors (nAChRs) on striatal synaptosomes stimulate dopamine release. Partial inhibition by the alpha3beta2-selective alpha-conotoxin-MII indicates heterogeneity of presynaptic nAChRs on dopamine terminals. We have used this alpha-conotoxin and UB-165, a novel hybrid of epibatidine and anatoxin-a, to address the hypothesis that the alpha-conotoxin-MII-insensitive subtype is composed of alpha4 and beta2 subunits. UB-165 shows intermediate potency, compared with the parent molecules, at alpha4beta2* and alpha3-containing binding sites, and resembles epibatidine in its high discrimination of these sites over alpha7-type and muscle binding sites. (+/-)-Epibatidine, (+/-)-anatoxin-a, and (+/-)-UB-165 stimulated [(3)H]-dopamine release from striatal synaptosomes with EC(50) values of 2.4, 134, and 88 nM, and relative efficacies of 1:0.4:0.2, respectively. alpha-Conotoxin-MII inhibited release evoked by these agonists by 48, 56, and 88%, respectively, suggesting that (+/-)-UB-165 is a very poor agonist at the alpha-conotoxin-MII-insensitive nAChR subtype. In assays of (86)Rb(+) efflux from thalamic synaptosomes, a model of an alpha4beta2* nAChR response, (+/-)-UB-165 was a very weak partial agonist; the low efficacy of (+/-)-UB-165 at alpha4beta2 nAChR was confirmed in Xenopus oocytes expressing various combinations of human nAChR subunits. In contrast, (+/-)-UB-165 and (+/-)-anatoxin-a were similarly efficacious and similarly sensitive to alpha-conotoxin-MII in increasing intracellular Ca(2+) in SH-SY5Y cells, a functional assay for native alpha3-containing nAChR. These data support the involvement of alpha4beta2* nAChR in the presynaptic modulation of striatal dopamine release and illustrate the utility of exploiting a novel partial agonist, together with a selective antagonist, to dissect the functional roles of nAChR subtypes in the brain.
