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willardiine

Known as: (S)-alpha-amino-3,4-dihydro-2,4-dioxo-1(2H)-pyrimidine propanoic acid, 3-(Uracil-1-yl)-L-alanine, beta-(2,4-dihydroxypyrimidin-1-yl)alanine 
National Institutes of Health

Related topics

Related topics

3 relations

Broader (2)

AlanineUracil
analogs & derivatives

Papers overview

Semantic Scholar uses AI to extract papers important to this topic.
2009
2009
Mechanisms of antagonism of the GluR2 AMPA receptor: structure and dynamics of the complex of two willardiine antagonists with the glutamate binding domain.
Ionotropic glutamate receptors mediate the majority of vertebrate excitatory synaptic transmission. The development of selective… 
Highly Cited
2008
Highly Cited
2008
Mechanism of partial agonism at the GluR2 AMPA receptor: Measurements of lobe orientation in solution.
The mechanism by which the binding of a neurotransmitter to a receptor leads to channel opening is a central issue in molecular… 
Highly Cited
2007
Highly Cited
2007
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and…
Some N3-substituted analogues of willardiine such as 11 and 13 are selective kainate receptor antagonists. In an attempt to… 
Highly Cited
2006
Highly Cited
2006
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.
N3-substitution of the uracil ring of willardiine with a variety of carboxyalkyl or carboxybenzyl substituents produces AMPA and… 
2005
2005
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
The natural product willardiine (8) is an AMPA receptor agonist while 5-iodowillardiine (10) is a selective kainate receptor… 
Highly Cited
2004
Highly Cited
2004
Characterisation of UBP296: a novel, potent and selective kainate receptor antagonist
1998
1998
Pharmacological differentiation of kainate receptors on neonatal rat spinal motoneurones and dorsal roots
Highly Cited
1997
Highly Cited
1997
Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.
Both willardiine and azawillardiine analogs (18-28) have been reported to be potent and selective agonists for either AMPA or… 
Highly Cited
1994
Highly Cited
1994
Willardiines differentiate agonist binding sites for kainate- versus AMPA-preferring glutamate receptors in DRG and hippocampal neurons
Concentration jump responses to 5-substituted (S)-willardiines were recorded from dorsal root ganglion (DRG) and hippocampal… 
Highly Cited
1992
Highly Cited
1992
Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine
Willardiine [(S)-1-(2-amino-2-carboxyethyl)pyrimidine-2,4-dione] is a naturally occurring heterocyclic excitatory amino acid… 
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