S-8510 free base

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 530313

CAS#: 151224-83-8 (free base)

Description: S-8510, also known as SB-737552, is a GABA-A receptor inverse agonist potentially for the treatment of dementia. S-8510 ameliorated memory impairment induced by cholinergic deficit in the water maze paradigm of Wistar rats. S-8510 augmented LTP of the Schaffer collateral/commissural fiber-CA1 synapses in the hippocampal slice preparations of SD rat. S-8510 increased the extracellular levels of acetylcholine and noradrenaline in the hippocampus of Wistar rat. S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimal electroconvulsive shock- or strychnine-induced convulsion in ddY mice.


Price and Availability

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S-8510 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 530313
Name: S-8510 free base
CAS#: 151224-83-8 (free base)
Chemical Formula: C12H10N4O2
Exact Mass: 242.0804
Molecular Weight: 242.238
Elemental Analysis: C, 59.50; H, 4.16; N, 23.13; O, 13.21


Synonym: S-8510; SB-737552; S8510; SB737552; S 8510; SB 737552.

IUPAC/Chemical Name: 2-(isoxazol-3-yl)-1,6,7,9-tetrahydroimidazo[4,5-d]pyrano[4,3-b]pyridine

SMILES Code: C12=NC=C3C(NC(C4=NOC=C4)=N3)=C1COCC2


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

Related CAS#
151224-83-8 (S-8510 Free)
365279-39-6 (S-8510 phosphoric acid salt)


References

1: Chorvat RJ, Zaczek R, Brown BS. Ion channel modulators that enhance acetylcholine release: potential therapies for Alzheimer's disease. Expert Opin Investig Drugs. 1998 Apr;7(4):499-518. PubMed PMID: 15991988.

2: Kominami G, Nakamura M, Chomei N, Takada S. Radioimmunoassay for a novel benzodiazepine inverse agonist, S-8510, in human plasma and urine. J Pharm Biomed Anal. 1999 Jun;20(1-2):145-53. PubMed PMID: 10704018.

3: Tanaka H, Mizojiri K. Drug-protein binding and blood-brain barrier permeability. J Pharmacol Exp Ther. 1999 Mar;288(3):912-8. PubMed PMID: 10027826.

4: Abe K, Sawada T, Horiuchi M, Yoshimura K. Effects of S-8510, a benzodiazepine receptor partial inverse agonist, on event-related potentials (P300) in monkeys. Psychopharmacology (Berl). 1999 Jan;141(1):71-6. PubMed PMID: 9952067.

5: Abe K, Takeyama C, Yoshimura K. Effects of S-8510, a novel benzodiazepine receptor partial inverse agonist, on basal forebrain lesioning-induced dysfunction in rats. Eur J Pharmacol. 1998 Apr 24;347(2-3):145-52. PubMed PMID: 9653874.

6: Nezasa K, Higaki K, Takeuchi M, Yukawa T, Nakano M. Pharmacokinetics of a novel benzodiazepine partial inverse agonist in the F344 rat, SD rat and B6C3F1 mouse. Xenobiotica. 1998 May;28(5):515-25. PubMed PMID: 9622853.

7: Kawasaki K, Eigyo M, Ikeda M, Kihara T, Koike K, Matsushita A, Murata S, Shiomi T, Takada S, Yasui M. A novel benzodiazepine inverse agonist, S-8510, as a cognitive enhancer. Prog Neuropsychopharmacol Biol Psychiatry. 1996 Nov;20(8):1413-25. PubMed PMID: 9004347.

8: Takada S, Sasatani T, Chomei N, Adachi M, Fujishita T, Eigyo M, Murata S, Kawasaki K, Matsushita A. Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands. J Med Chem. 1996 Jul 5;39(14):2844-51. PubMed PMID: 8709114.