Delving into the Latest Updates on WLB-87848 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

σ1 receptor

Action

agonists

Mechanism

σ1 receptor agonists(Sigma opioid receptor agonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Memory Disorders

Inactive Indication-

Originator Organization

WeLab Barcelona

Active Organization

WeLab Barcelona

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC17H15F2N3OS

InChIKeyIKJZVJSFYFMWTK-SECBINFHSA-N

CAS Registry2839205-09-1

The synthesis and pharmacological activity of a new series of thieno[2,3-d]pyrimidin-4(3H)-one derivatives as sigma-1 receptor (σ₁R) ligands are reported. A hit from a high-throughput screening program was evolved into a highly potent and selective σ₁R agonist (14qR) that contains a free NH group as positive ionizable moiety, not fulfilling the usual pharmacophoric features of the σ₁R. The compound shows good physicochemical and ADMET characteristics, displays an agonist profile in the binding immunoglobulin protein/σ₁R association assay, induces neuron viability in an in vitro model of β-amyloid peptide intoxication, and presents positive results against recognition memory impairment induced by hippocampal injection of Aβ peptide in rats after oral treatment, altogether making 14qR (WLB-87848) an interesting candidate for neuroprotection.

100 Deals associated with WLB-87848

Login to view more data