A 841720 |
Catalog No.GC16068 |
mGluR1 antagonist, non-competitive
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 869802-58-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
A 841720 is a novel non-competitive antagonist of metabotropic glutamate receptor 1 (mGluR1), with an IC50 value of 10.7 nM to 10 µM L-glutamate-induced calcium release at human mGluR1 receptors [1].
Glutamate as the major excitatory neurotransmitter in the central nervous system functions through two types of receptors, ionotropic glutamate receptors and metabotropic glutamate receptors (mGluRs). MGluRs includes group I mGluRs (mGluR1 and mGluR5 receptors), group II (mGluR2 and mGluR3 receptors) and group III (mGluR4, 6, 7, 8 receptors) [1].
In cells, agonist-induced calcium release was concentration-dependently inhibited by A 841720 in a human mGluR5 receptor FLIPR functional assay. But the IC50 value was just 343 nM. In cells expressing recombinant mGluR5 receptors, A 841720 did not block agonist-induced response. In the human mGluR1 receptor FLIPR assay, the log concentration-response curve was shifted by A 841720 at 10 nM to the right. A 841720 at increasing concentrations profoundly reduced the amplitude of L-quisqualate-evoked calcium release. A 841720 at 30 nM reduced the maximal agonist-induced response by 38%. L-quisqualate-induced response was completely abolished by A 841720 at 100 nM [1].
In a water maze test, all rats gradually learned to locate the submerged platform. Treatment with A 841720 significantly slowered rats to find the platform than vehicle control rats. Rats treated with A 841720 at both 30 and 100 µmol/kg doses not only significantly traveled longer distance to find the hidden platform, but also significantly spent longer time to reach the platform [1].
Reference:
[1]. El-Kouhen O, Lehto SG, Pan JB, et al. Blockade of mGluR1 receptor results in analgesia and disruption of motor and cognitive performances: effects of A-841720, a novel non-competitive mGluR1 receptor antagonist. British journal of pharmacology, 2006, 149(6): 761-774.
Cas No. | 869802-58-4 | SDF | |
Chemical Name | 3-(azepan-1-yl)-9-(dimethylamino)pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4(3H)-one | ||
Canonical SMILES | O=C(C(SC1=NC=CC(N(C)C)=C21)=C2N=C3)N3N4CCCCCC4 | ||
Formula | C17H21N5OS | M.Wt | 343.45 |
Solubility | DMF: 16 mg/ml,DMSO: 25 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 3 mg/ml | Storage | Store at RT |
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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.9116 mL | 14.5582 mL | 29.1163 mL |
5 mM | 0.5823 mL | 2.9116 mL | 5.8233 mL |
10 mM | 0.2912 mL | 1.4558 mL | 2.9116 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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