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XB-ART-5298
J Med Chem May 22, 2003; 46 (11): 2246-9.

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).

Bjerrum EJ , Kristensen AS , Pickering DS , Greenwood JR , Nielsen B , Liljefors T , Schousboe A , Bräuner-Osborne H , Madsen U .


Abstract
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.

PubMed ID: 12747796
Article link: J Med Chem

Genes referenced: gria1 gria3



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