S-8510 phosphate
S-8510 (phosphate) is an inverse Benzodiazepine (BDZ) receptor agonist, with Kis of 34.6 nM, 36.2 nM for –GABA and +GABA respectively.
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- CAS No.: 151466-23-8
- Formule: C12H13N4O6P
- Masse moléculaire:340.23
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Ki: 34.6 nM (-GABA), 36.2 nM (+GABA)[1].
S-8510 has a relatively high affinity to BDZ receptors. The ratio of Ki values for each ligand with and without GABA is defined as the GABA ratio, which is considered as a biochemical index for BDZ receptor ligands. The GABA ratio for S-8510 or CGS8216 is close to the value for flumazenil which is considered as an antagonist or a very weak agonist. S-8510 (10-7 M) enhances LTP and this enhancement is antagonized by BDZ receptor antagonist, flumazenil. Flumazenil itself does not atfect LTP or evokes responses prior to tetanic stimulation. S-8510 has no effect on the field evoked potential up to 10-5 M. However, S-8510 increases the amplitude of the population spike at a dose of 10-4 M, and this effect is completely antagonized by concomitant application of flumazenil (10-4 M) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 151466-23-8
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Masse moléculaire 340.23
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Formule C12H13N4O6P
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SMILES
O=P(O)(O)O.C12=NC=C3C(NC(C4=NOC=C4)=N3)=C1COCC2
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Synonyms
SB-737552 phosphate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
Mice, Rats[1]
Proconvulsant actions of S-8510 are examined in combiition with a subconvulsive dose of convulsant (PTZ or strychnine) or minimal electroconvulsive shock in ddY mice. Each convulsant is administrated, simultaneously with the inverse agonist, whereas minimal electroconvulsive shock is applied 5 min after intravenous injection of the inverse agonist. The proconvulsant test of S-8510 on PTZ (52, 62.5, 75 or 90 mg/kg s.c.) or strychnine (0.25 mg/kg, s.c.)-induced convulsion is made. ED50 values for producing clonic convulsion to death in 50% of ddY mice are calculated. Anxiogenic actions of each inverse agonist are examined in the punished water licking method in Wistar rats. Each inverse agonist is administered per OS 30 min before the test trial. Antiamnesic actions of inverse agonists are examined in the water maze paradigm. Wistar rats are given 4 trials every day for consecutive 4 days. On the 5 th day, each animal has the retention test for 60 s. Amnesia is produced by intraperitoneally injected scopolamine at a dose of 0.5 mg/kg. Scopolamine and each inverse agonist are given 15 min and 30 min before the retention trial, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)