MDL 105519 |
カタログ番号GC30951 |
MDL 105519 は、NMDA 受容体に結合するグリシンの強力かつ選択的なアンタゴニストです。
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Cas No.: 161230-88-2
Sample solution is provided at 25 µL, 10mM.
MDL 105519 is a potent and selective antagonist of glycine binding to the NMDA receptor.
MDL 105519 is a potent and selective ligand for the glycine recognition site that completely inhibit the binding of [3H]glycine to rat brain membranes with a Ki value of 10.9 nM. MDL 105519 is approximately 10,000-fold selective for the glycine recognition site relative to the other receptor types investigated. MDL 105519 inhibits NMDA-dependent responses, such as elevations of [3H]TCP binding in brain membranes, cyclic GMP accumulation in brain slices, and alterations in cytosolic Ca2+ and Na+-Ca2+ currents in cultured neurons. Inhibition is non-competitive with respect to NMDA and could be nullified with D-serine[1].
MDL 105519 is an NMDA receptor antagonist in vivo. Intravenously administration of MDL 105519 prevents harmaline-stimulated increases in cerebellar cyclic GMP content, providing biochemical evidence of NMDA receptor antagonism in vivo. This antagonism is associated with anticonvulsant activity in genetically based, chemically induced, and electrically mediated seizure models. Anxiolytic activity is observed in the rat separation-induced vocalization model, but muscle-relaxant activity is apparent at lower doses. Higher doses impair rotorod performance, but are without effect on mesolimbic dopamine turnover or prepulse inhibition of the startle reflex[1].
[1]. Baron BM, et al. Pharmacological characterization of MDL 105,519, an NMDA receptor glycine site antagonist. Eur J Pharmacol. 1997 Apr 4;323(2-3):181-92.
Animal experiment: | Adult, male, CD rats are administered MK-801 (n=4, 2 mg/kg, i.p.) or MDL 105519 (n=4, 2 mg/kg, i.p.) and extracellular dopamine concentrations are measured using in vivo microdialysis[1]. Mice: Mice adult male CD-1 are injected with various doses of MDL 105519 (8, 16, 32, 64, 128 mg/kg) intraperitoneally and 30 min later are administered harmaline 50 mg/kg. Sixty minutes after the first injection, the mice are killed and cerebellar cGMP content is measured by radioimmunoassay[1]. |
References: [1]. Baron BM, et al. Pharmacological characterization of MDL 105,519, an NMDA receptor glycine site antagonist. Eur J Pharmacol. 1997 Apr 4;323(2-3):181-92. |
Cas No. | 161230-88-2 | SDF | |
Canonical SMILES | O=C(O)C(N1)=C(/C=C(C2=CC=CC=C2)/C(O)=O)C3=C1C=C(Cl)C=C3Cl | ||
Formula | C18H11Cl2NO4 | M.Wt | 376.19 |
溶解度 | DMSO : 17 mg/mL (45.19 mM) | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.6582 mL | 13.2912 mL | 26.5823 mL |
5 mM | 0.5316 mL | 2.6582 mL | 5.3165 mL |
10 mM | 0.2658 mL | 1.3291 mL | 2.6582 mL |
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- Purity: >98.00%
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Average Rating: 5
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