S-8510 free base

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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.


Chemical Structure

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S-8510 free base
CAS# 151224-83-8 (free base)

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

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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

InChi Key: ITPFSYAYHHPKRT-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H10N4O2/c1-3-17-6-7-8(1)13-5-10-11(7)15-12(14-10)9-2-4-18-16-9/h2,4-5H,1,3,6H2,(H,14,15)

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

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).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 242.238 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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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.



Additional Information

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