[3H]ATPA: a high affinity ligand for GluR5 kainate receptors
| Autor: | Calvin R. Hawes, Michele Deverill, Gareth J. Ellis, Ken Hoo, David Bleakman, Povl Krogsgaard-Larsen, Beatta Legutko, Tine B. Stensbøl, Geihan Rizkalla, Phil Skolnick |
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| Rok vydání: | 1999 |
| Předmět: |
Agonist
Stereochemistry medicine.drug_class Kainate receptor AMPA receptor Biology Cell Line Cellular and Molecular Neuroscience Receptors Kainic Acid Ganglia Spinal Radioligand medicine Excitatory Amino Acid Agonists Animals Humans Receptor Pharmacology Neurons Kainic Acid Glutamate receptor Isoxazoles Ligand (biochemistry) Rats Membrane Animals Newborn Propionates |
| Zdroj: | Neuropharmacology. 38(12) |
| ISSN: | 0028-3908 |
| Popis: | The pharmacological properties of [ 3 H]ATPA (( RS )-2-amino-3(3-hydroxy-5-tert-butylisoxazol-4-yl)propanoic acid) are described. ATPA is a tert -butyl analogue of AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazoleproprionic acid) that has been shown to possess high affinity for the GluR5 subunit of kainate receptors. [ 3 H]ATPA exhibits saturable, high affinity binding to membranes expressing human GluR5 (GluR5) kainate receptors ( K d ∼13 nM). No specific binding was observed in membranes expressing GluR2 and GluR6 receptors. Several compounds known to interact with the GluR5 kainate receptor inhibited [ 3 H]ATPA binding with potencies similar to those obtained for competition of [ 3 H]kainate binding to GluR5. Saturable, high affinity [ 3 H]ATPA binding ( K d ∼4 nM) was also observed in DRG neuron (DRG) membranes isolated from neonatal rats. The rank order potency of compounds to inhibit [ 3 H]ATPA binding in rat DRG and GluR5 membranes were in agreement. These finding demonstrate that [ 3 H]ATPA can be used as a radioligand to examine the pharmacological properties of GluR5 containing kainate receptors. |
| Databáze: | OpenAIRE |
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