Drug intelligence / Profile preview

willardiine

Development stage
Unknown
Modality
Small Molecules
01

Overview

Willardiine is a naturally occurring amino acid derivative isolated from the seeds of Acacia willariana. It acts as a partial agonist at ionotropic glutamate receptors—specifically the non-NMDA subtypes AMPA and kainate receptors. These receptors are found at excitatory synapses in the central nervous system and mediate fast synaptic transmission by binding glutamate or structurally similar ligands such as willardiine. Activation of these receptors by willardiine leads to an influx of positive ions into neurons and subsequent neural depolarization. Willardiine has been primarily used as a research tool to study receptor structure and function; it is not approved for therapeutic use in any indication[1][2]. Only the (S)-isomer binds effectively to AMPA/kainate receptors[2]. Overactivation can cause neurotoxicity, but at typical research concentrations, toxicity is low[2].

Other names
beta-(2,4-dihydroxypyrimidin-1-yl)alanine3-(1-uracyl)-L-alanine(S)-willardiineL-willardiine
02

Targets

Kainate-type ionotropic glutamate receptorAMPAR (AMPA receptor)

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