Characterization of [3H]MEN 11420, a Novel Glycosylated Peptide Antagonist Radioligand of the Tachykinin NK2Receptor
| Autor: | Anna-Rita Renzetti, A. Lippi, Marco Guelfi, Paola Cucchi, Marco Criscuoli, Carlo Alberto Maggi, R.-M. Catalioto, Laura Quartara |
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| Rok vydání: | 1998 |
| Předmět: |
medicine.medical_specialty
animal structures High affinity binding Biophysics Peptide CHO Cells Transfection Binding Competitive Peptides Cyclic digestive system Biochemistry Radioligand Assay Cricetinae Tachykinins Internal medicine Radioligand medicine Animals Humans Potency Receptor Molecular Biology chemistry.chemical_classification Binding Sites Chemistry Chinese hamster ovary cell Antagonist Receptors Neurokinin-2 Cell Biology Kinetics Endocrinology |
| Zdroj: | Biochemical and Biophysical Research Communications. 248:78-82 |
| ISSN: | 0006-291X |
| Popis: | [ 3 H]MEN 11420, a radiolabeled glycosylated peptide antagonist of the tachykinin NK 2 receptor, has been investigated in ligand-receptor binding assays using membranes of CHO cells transfected with the human tachykinin NK 2 receptor. [ 3 H]MEN 11420 bound to a single class of high affinity binding sites: its binding was inhibited by natural tachykinins (potency ranking: NKA ⪢ SP ≥ NKB), as well as by peptide (MEN 11420 > MEN 10376 ⪢ R 396) and nonpeptide (SR 48968 > GR 159897) selective NK 2 receptor antagonists. These data indicate that [ 3 H]MEN 11420 is a potent radioligand for the human tachykinin NK 2 receptor that may represent a useful tool for studying ligand-receptor interactions at the molecular level. |
| Databáze: | OpenAIRE |
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