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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
11
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pubmed:dateCreated |
2003-5-15
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pubmed:abstractText |
On the basis of structural studies, chloro-homoibotenic acid (Cl-HIBO) was designed and synthesized. Cl-HIBO was characterized in binding and electrophysiology experiments on native and cloned subtypes of GluRs. Electrophysiological selectivities ranged from 275 to 1600 for GluR1/2 over GluR3/4. The potent AMPA receptor activity was strongly desensitizing and the neurotoxicity similar to AMPA. Thus, Cl-HIBO is the most subtype selective agonist reported to date on GluR1/2, and offers a new standard for selectively studying subtypes of AMPA receptors.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
22
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pubmed:volume |
46
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2246-9
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:12747796-Animals,
pubmed-meshheading:12747796-Cell Survival,
pubmed-meshheading:12747796-Cells, Cultured,
pubmed-meshheading:12747796-Cerebral Cortex,
pubmed-meshheading:12747796-Electrophysiology,
pubmed-meshheading:12747796-Excitatory Amino Acid Agonists,
pubmed-meshheading:12747796-Isoxazoles,
pubmed-meshheading:12747796-Mice,
pubmed-meshheading:12747796-Models, Molecular,
pubmed-meshheading:12747796-Neurons,
pubmed-meshheading:12747796-Oocytes,
pubmed-meshheading:12747796-Propionates,
pubmed-meshheading:12747796-Propionic Acids,
pubmed-meshheading:12747796-Radioligand Assay,
pubmed-meshheading:12747796-Rats,
pubmed-meshheading:12747796-Receptors, AMPA,
pubmed-meshheading:12747796-Receptors, Metabotropic Glutamate,
pubmed-meshheading:12747796-Stereoisomerism,
pubmed-meshheading:12747796-Structure-Activity Relationship,
pubmed-meshheading:12747796-Xenopus laevis
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pubmed:year |
2003
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pubmed:articleTitle |
Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO).
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pubmed:affiliation |
Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, 2 Universitetsparken, DK-2100 Copenhagen, Denmark.
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pubmed:publicationType |
Journal Article,
In Vitro,
Research Support, Non-U.S. Gov't
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