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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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, Esben J; Kristensen, Anders S; Pickering, Darryl S; Greenwood, Jeremy R; Nielsen, Birgitte; Liljefors, Tommy; Schousboe, Arne; Bräuner-Osborne, Hans; Madsen, Ulf; Pickering, Darryl.
In: Journal of Medicinal Chemistry, Vol. 46, No. 11, 2003, p. 2246-9.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - 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)
AU - Bjerrum, Esben J
AU - Kristensen, Anders S
AU - Pickering, Darryl S
AU - Greenwood, Jeremy R
AU - Nielsen, Birgitte
AU - Liljefors, Tommy
AU - Schousboe, Arne
AU - Bräuner-Osborne, Hans
AU - Madsen, Ulf
AU - Pickering, Darryl
N1 - Keywords: Animals; Cell Survival; Cells, Cultured; Cerebral Cortex; Electrophysiology; Excitatory Amino Acid Agonists; Isoxazoles; Mice; Models, Molecular; Neurons; Oocytes; Propionates; Propionic Acids; Radioligand Assay; Rats; Receptors, AMPA; Receptors, Metabotropic Glutamate; Stereoisomerism; Structure-Activity Relationship; Xenopus laevis
PY - 2003
Y1 - 2003
N2 - 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.
AB - 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.
U2 - 10.1021/jm020588f
DO - 10.1021/jm020588f
M3 - Journal article
C2 - 12747796
VL - 46
SP - 2246
EP - 2249
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 11
ER -
ID: 20122633