Drug intelligence / Profile preview

ly404187

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

Overview

LY404187 is a selective, potent, and centrally active **positive allosteric modulator of AMPA receptors**. It belongs to the biarylpropylsulfonamide class of AMPA receptor potentiators. LY404187 preferentially enhances recombinant human homomeric GluR2 and GluR4 subunits of AMPA receptors, potentiating the flip splice variants more strongly than the flop variants. Its action involves suppressing desensitization of the ion channels and augmenting glutamatergic synaptic transmission. LY404187 increases excitatory neurotransmission, indirectly recruits NMDA receptor activity, and elevates BDNF levels in the brain. It has demonstrated efficacy in animal models to enhance cognitive function, display potential antidepressant action, and show possible applications in treating schizophrenia, Parkinson's disease, and ADHD. The drug was developed by Eli Lilly and Company and remains experimental with preclinical evidence for neurotrophic and cognitive-enhancing effects[1][3][6].

Other names
LY404187LY-404187LY 404187
02

Targets

AMPAR (AMPA receptor)

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