Willardiine
Willardiine (correctly spelled with two successive i's) or ("S")-1-(2-amino-2-carboxyethyl)pyrimidine-2,4-dione is a chemical compound that occurs naturally in the seeds of "Mariosousa willardiana" and "Acacia" sensu lato. The seedlings of these plants contain enzymes capable of complex chemical substitutions that result in the formation of free amino acids ("See:" #Synthesis). Willardiine is frequently studied for its function in higher level plants. Additionally, many derivates of willardiine are researched for their potential in pharmaceutical development. Willardiine was first discovered in 1959 by R. Gmelin, when he isolated several free, non-protein amino acids from "Acacia willardiana" (another name for "Mariosousa willardiana") when he was studying how these families of plants synthesize uracilyalanines. A related compound, Isowillardiine, was concurrently isolated by a different group, and it was discovered that the two compounds had different structural and functional properties. Subsequent research on Willardiine has focused on the functional significance of different substitutions at the nitrogen group and the development of analogs of Willardiine with different pharmacokinetic properties. In general, Willardiine is the one of the first compounds studied in which slight changes to molecular structure result in compounds with significantly different pharmacokinetic properties.

Willardiine is a partial agonist of Ionotropic glutamate receptors. These receptors are found at excitatory synapses and bind glutamate (the major excitatory neurotransmitter) and structurally similar ligands, such as Willardiine. Receptor activation leads to influx of positive ions into the neuron, resulting in neural depolarization ("See:" #Structure and Activity). Willardiine specifically agonizes non-NMDA glutamate receptors: AMPA and kainate receptors.

Willardiine analogs have been developed that have different binding affinities for the AMPA and kainate receptors. These analogs have been used to study the structure of these receptors, as well as the functional significance of receptor activation in different brain regions. While Willardiine and its analogs have not been explicitly studied as therapeutics, there are a variety of neurological disorders characterized by alterations in glutamate signaling, and ligands for AMPA and kainate receptors are often studied as potential therapeutics.
Q11173
chemical compound
Concept
Q4671022
Mariosousa willardiana
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Q21823316
"Acacia" sensu lato
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Q1385709
seedling
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Q8047
enzyme
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Q503396
chemical substitution
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Q8066
amino acid
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None
#Synthesis
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Q12140
pharmaceutical
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Q627
nitrogen
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Q3827885
analogs
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Q323936
pharmacokinetic
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Q770260
partial agonist
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Q24779507
Ionotropic glutamate receptor
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Q5419646
excitatory synapse
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Q1532394
glutamate
UNK
Q162657
neurotransmitter
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Q193161
ligand
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Q36496
positive ions
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Q43054
neuron
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Q83183
depolarization
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None
#Structure and Activity
UNK
Q414896
NMDA glutamate receptor
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Q66370552
AMPA
MISC
Q390239
kainate
Concept
Q3339235
neurological disorder
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Q420510
glutamate signaling
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Q12093199
Willardiine
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Q12093199
Willardiine
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Q12093199
Willardiine
Concept
Q12093199
Willardiine
Concept
Q12093199
Willardiine
Concept
Q12093199
Willardiine
Concept
Q12093199
Willardiine
Concept
Q12093199
Willardiine
Concept
Q12093199
Willardiine
Concept
Q12093199
Willardiine
Concept
Q12093199
Willardiine
Concept
1959-01-01T00:00:00Z^^http://www.w3.org/2001/XMLSchema#dateTime
1959
DATE
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-1
NUMBER
+2^^http://www.w3.org/2001/XMLSchema#decimal
2
NUMBER
-2^^http://www.w3.org/2001/XMLSchema#decimal
-2
NUMBER
-2.4^^http://www.w3.org/2001/XMLSchema#decimal
-2,4
NUMBER
instance of