Characterization of the Binding Sites of [3H]SR 48968, a Potent Nonpeptide Radioligand Antagonist of the Neurokinin-2 Receptor
| Autor: | P. Pointeau, J.C. Breliere, F. Golliot, X. Emondsalt, G. Lefur |
|---|---|
| Rok vydání: | 1993 |
| Předmět: |
Duodenum
Guinea Pigs Urinary Bladder Biophysics Hamster Peptide In Vitro Techniques Substance P Binding Competitive Biochemistry Rats Sprague-Dawley Piperidines Cricetinae Radioligand Animals Potency Binding site Receptor Molecular Biology chemistry.chemical_classification Binding Sites Mesocricetus Chemistry Antagonist Receptors Neurokinin-2 Cell Biology Molecular biology Rats Receptors Neurotransmitter Dissociation constant Kinetics Benzamides |
| Zdroj: | Biochemical and Biophysical Research Communications. 191:1172-1177 |
| ISSN: | 0006-291X |
| DOI: | 10.1006/bbrc.1993.1340 |
| Popis: | [3H]SR 48968, a radiolabeled nonpeptide antagonist of NK-2 receptor, has been tested in ligand-receptor binding assays using rat duodenum, hamster urinary bladder and guinea pig ileum membranes. [3H]SR 48968 bound to a single class of high affinity binding sites. Its affinity was slightly species-dependent. Its binding was inhibited by neurokinins, following the rank order of potency NKA > NKB > SP. It was also inhibited by peptide antagonists of NK-2 receptor (MEN 10,376, L 659,877), but their relative potencies were highly species-dependent. Unlabeled SR 48968, but not its R-enantiomer (SR 48965), also potently inhibited its binding. These data show that [3H]SR 48968 potently binds to NK-2 receptor and therefore is a useful tool to study NK-2 receptor. |
| Databáze: | OpenAIRE |
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