[3H]Propyl-6-azido-β-carboline-3-carboxylate: a new photoaffinity label for the GABAA-benzodiazepine receptor
Autor: | Robert H. Dodd, Werner Sieghart, Jürgen Zezula, Susanne Karall |
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Rok vydání: | 1995 |
Předmět: |
Stereochemistry
Biology Tritium Binding Competitive Radioligand Assay chemistry.chemical_compound medicine Animals Carboxylate Receptor Brain Chemistry Pharmacology Diazepam GABAA receptor Ligand Brain Affinity Labels Receptors GABA-A In vitro Rats Kinetics chemistry Biochemistry Flunitrazepam Gabaa benzodiazepine receptor Carbolines medicine.drug |
Zdroj: | European Journal of Pharmacology. 281:93-96 |
ISSN: | 0014-2999 |
DOI: | 10.1016/0014-2999(95)00284-r |
Popis: | [ 3 H]Propyl-6-azido-β-carboline-3-carboxylate ([ 3 H]ACCP) exhibited a high affinity for GABA A receptors affinity purified from the brains of adult rats, and binding of this compound could be inhibited by several ligands of the benzodiazepine binding site of GABA A receptors. On irradiation with UV light, [ 3 H]ACCP, similarly to [ 3 H]flunitrazepam, irreversibly labeled a protein with an apparent molecular weight of 51 kDa in affinity-purified GABA A receptors, and this labeling could be inhibited in the presence of diazepam. These data indicate that [ 3 H]ACCP can be used as a photoaffinity label for GABA A receptors. |
Databáze: | OpenAIRE |
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