Talsupram hydrochlorideSelective inhibitor of noradrenalin transporters CAS# 25487-28-9 |
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Quality Control & MSDS
3D structure
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| Cas No. | 25487-28-9 | SDF | Download SDF |
| PubChem ID | 33013 | Appearance | Powder |
| Formula | C20H26ClNS | M.Wt | 347.95 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 20 mM in water and to 100 mM in DMSO | ||
| Chemical Name | 1,3-Dihydro-N,3,3-trimethyl-1-pheny | ||
| SMILES | [Cl-].C[NH2+]CCCC1(SC(C)(C)c2ccccc12)c3ccccc3 | ||
| Standard InChIKey | YMZCMCDSCRSIBS-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C20H25NS.ClH/c1-19(2)17-12-7-8-13-18(17)20(22-19,14-9-15-21-3)16-10-5-4-6-11-16;/h4-8,10-13,21H,9,14-15H2,1-3H3;1H | ||
| 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 | Selective noradrenalin re-uptake inhibitor; exhibits a high affinity for the human noradrenalin transporter (NET) against SERT and DAT (IC50 values are 0.79, 850 and 9300 nM for inhibition of monoamine uptake by NET, SERT and DAT respectively). Antidepressant. |
Talsupram hydrochloride Dilution Calculator
Talsupram hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.874 mL | 14.3699 mL | 28.7398 mL | 57.4795 mL | 71.8494 mL |
| 5 mM | 0.5748 mL | 2.874 mL | 5.748 mL | 11.4959 mL | 14.3699 mL |
| 10 mM | 0.2874 mL | 1.437 mL | 2.874 mL | 5.748 mL | 7.1849 mL |
| 50 mM | 0.0575 mL | 0.2874 mL | 0.5748 mL | 1.1496 mL | 1.437 mL |
| 100 mM | 0.0287 mL | 0.1437 mL | 0.2874 mL | 0.5748 mL | 0.7185 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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Synthesis and biological evaluation of [11C]talopram and [11C]talsupram: candidate PET ligands for the norepinephrine transporter.[Pubmed:15246361]
Nucl Med Biol. 2004 Aug;31(6):705-18.
PET and SPECT ligands for the norepinephrine transporter (NET) will be important tools for studying the physiology, pathophysiology and pharmacology of the CNS noradrenergic system in vivo. A series of candidate NET ligands were synthesized and characterized in terms of their affinity for human monoamine transporters. The two most promising compounds, talopram and talsupram, were radiolabeled with carbon-11 and evaluated through biodistribution studies in rats and PET imaging studies in a rhesus monkey. Although both compounds displayed high affinity and selectivity for the human NET in vitro, these compounds did not enter the CNS in adequate amounts to be used in PET imaging studies.
Cocaine-like discriminative stimulus effects of heroin: modulation by selective monoamine transport inhibitors.[Pubmed:14985417]
J Pharmacol Exp Ther. 2004 Jul;310(1):342-8.
In previous studies, heroin was shown to engender cocaine-like discriminative stimulus (DS) effects; however, the mechanisms underlying the cocaine-like effects of heroin are unknown. The present study evaluated the extent to which the shared DS effects of heroin and cocaine involve common monoaminergic mechanisms of action. In squirrel monkeys discriminating cocaine (0.3 mg/kg) from saline, heroin engendered full or partial substitution for cocaine in three of four monkeys. Pretreatment with the selective dopamine transport inhibitor 1-(2-[bis(4-fluorophenyl)methoxy]ethyl)-4-(3-phenylpropyl)piperazine (GBR 12909) dose dependently enhanced the cocaine-like DS effects of heroin in these three monkeys as well as the DS effects of cocaine in all subjects. Neither talsupram, a noradrenergic transport inhibitor, nor prazosin, a noradrenergic antagonist selective for alpha-1 receptors, systematically altered the cocaine-like DS effects of heroin at doses that enhanced (talsupram) or attenuated (prazosin) the DS effects of cocaine. Pretreatment with the serotonin uptake inhibitor citalopram similarly failed to alter the cocaine-like DS effects of heroin at doses that attenuated the DS effects of cocaine. Altogether, these findings suggest that heroin shares DS effects with cocaine in a subset of monkeys, and these cocaine-like effects are mediated at least in part by enhanced dopaminergic activity. Unlike the DS effects of cocaine itself, however, the cocaine-like DS effects of heroin do not appear to involve either noradrenergic or serotonergic mechanisms.
