TezampanelAMPA and receptor antagonist CAS# 154652-83-2 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 154652-83-2 | SDF | Download SDF |
| PubChem ID | 127894 | Appearance | Powder |
| Formula | C13H21N5O2 | M.Wt | 279.34 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO | ||
| Chemical Name | (3S,4aR,6R,8aR)-6-[2-(2H-tetrazol-5-yl)ethyl]-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid | ||
| SMILES | C1CC2CNC(CC2CC1CCC3=NNN=N3)C(=O)O | ||
| Standard InChIKey | ZXFRFPSZAKNPQQ-YTWAJWBKSA-N | ||
| Standard InChI | InChI=1S/C13H21N5O2/c19-13(20)11-6-10-5-8(1-3-9(10)7-14-11)2-4-12-15-17-18-16-12/h8-11,14H,1-7H2,(H,19,20)(H,15,16,17,18)/t8-,9+,10-,11+/m1/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. |
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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. | ||
Tezampanel Dilution Calculator
Tezampanel Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.5799 mL | 17.8993 mL | 35.7987 mL | 71.5973 mL | 89.4967 mL |
| 5 mM | 0.716 mL | 3.5799 mL | 7.1597 mL | 14.3195 mL | 17.8993 mL |
| 10 mM | 0.358 mL | 1.7899 mL | 3.5799 mL | 7.1597 mL | 8.9497 mL |
| 50 mM | 0.0716 mL | 0.358 mL | 0.716 mL | 1.4319 mL | 1.7899 mL |
| 100 mM | 0.0358 mL | 0.179 mL | 0.358 mL | 0.716 mL | 0.895 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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Tezampanel (LY293558) is a drug which acts as an antagonist at the AMPA and kainate families of ionotropic glutamate receptors, with selectivity for the GluR5 subtype of the kainate receptor. It has neuroprotective and anticonvulsant effects.
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Epidural tezampanel, an AMPA/kainate receptor antagonist, produces postoperative analgesia in rats.[Pubmed:17898404]
Anesth Analg. 2007 Oct;105(4):1152-9, table of contents.
BACKGROUND: We evaluated the epidural administration of Tezampanel, a non-N-methyl-d-aspartate receptor antagonist, in a rat model for postoperative pain. We sought to determine if this drug affects nociception when administered epidurally by testing its effects on responses to heat in normal rats. The effects of epidural Tezampanel on pain-related behaviors in rats that underwent plantar incision were also studied. METHODS: Rats were anesthetized and epidural catheters were placed. One day after epidural catheterization, the baseline heat withdrawal latency was measured. Epidural Tezampanel or morphine was tested for analgesia by examining their effects against heat withdrawal latency. Motor function was also tested. Comparisons to subcutaneous drug administration were made. Other rats underwent plantar incision after epidural catheterization to assess pain behavior caused by incision. The effects of epidural Tezampanel on the cumulative pain scoring, based on guarding, the withdrawal threshold to von Frey filament application, and the withdrawal latency to heat, were measured. The effects of epidural Tezampanel on arterial blood pressure and heart rate were also tested. RESULTS: Both epidural morphine and epidural Tezampanel increased withdrawal latency to heat. Only subcutaneous morphine affected heat withdrawal latency. After plantar incision, epidural Tezampanel decreased the median guarding pain score, increased the heat withdrawal latency and increased the mechanical withdrawal threshold indicating analgesic effects. Arterial blood pressure and heart rate did not change after epidural drug administration. CONCLUSION: These experiments demonstrate that epidural administration of Tezampanel produces analgesia to heat, motor side effects in some rats, and reduces pain behaviors caused by incision. No systemic analgesia was apparent using the largest dose.
