Drug intelligence / Profile preview

S-8510

Development stage
Unknown
Lead developer
Shionogi
Modality
Small Molecules
01

Overview

S-8510 is a small molecule benzodiazepine (BZD) receptor partial inverse agonist that acts at the BZD binding site of the GABA-A receptor in the central nervous system. As a partial inverse agonist and negative allosteric modulator of GABA-A receptors (distinct from full inverse agonists), it has lower efficacy and affinity for the BZD site. Preclinical studies indicate that S‑8510 can ameliorate memory impairment induced by cholinergic deficit and enhance long-term potentiation in hippocampal neurons. It increases extracellular acetylcholine and noradrenaline levels in the hippocampus without inducing anxiety or convulsions at therapeutic doses. The drug was primarily developed as a potential treatment for Alzheimer's disease and mild to moderate senile dementia[1][2][5].

Other names
S8510S-8510S 8510Imidazo(4,5-d)pyrano(4,3-b)pyridine, 1,6,7,9-tetrahydro-2-(3-isoxazolyl)-Imidazo(4,5-d)pyrano(4,3-b)pyridine, 3,6,7,9-tetrahydro-2-(3-isoxazolyl)-
02

Targets

BZD site (GABA-A receptor benzodiazepine site)

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