Drug intelligence / Profile preview

LY503430

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

LY503430 is a **small molecule drug** that acts as a **positive allosteric modulator of the AMPA receptor (Glutamate receptor ionotropic AMPA subunits A1–A4)**. It selectively enhances glutamate-induced responses at submicromolar concentrations in both recombinant and native neuronal preparations, increasing **synaptic transmission and plasticity**. LY503430 showed **neuroprotective and neurotrophic effects in rodent models of Parkinson’s disease**, including dose-dependent functional and histological protection against neurotoxicity, with additional increases in brain derived neurotrophic factor (BDNF) and growth associated protein-43 (GAP-43) expression. It has **good oral bioavailability** in preclinical species and was in development by **Eli Lilly** as a potential disease-modifying therapy for Parkinson’s disease[1][2][3][4][5][6].

Other names
LY503430LY-503430LY 503430(R)-4'-[1-fluoro-1-methyl-2-(propane-2-sulfonylamino)-ethyl]-biphenyl-4-carboxylic acid methylamide
02

Targets

GRIA1 (AMPA receptor subunit GluA1)GRIA4 (AMPA receptor subunit GluA4)GRIA2 (AMPA receptor subunit GluA2)GRIA3 (AMPA receptor subunit GluA3)

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