[3H]DuP 753, a highly potent and specific radioligand for the angiotensin II-1 receptor subtype
| Autor: | Andrew T. Chiu, Pieter B.M.W.M. Timmermans, Dale E. McCall, Paul E. Aldrich |
|---|---|
| Rok vydání: | 1990 |
| Předmět: |
medicine.medical_specialty
genetic structures medicine.drug_class Biophysics Tetrazoles Tritium Binding Competitive Biochemistry Losartan Microsomes Internal medicine medicine Radioligand Animals Binding site Receptor Molecular Biology Receptors Angiotensin Chemistry Angiotensin II Imidazoles Antagonist Cell Biology Ligand (biochemistry) Receptor antagonist Rats Kinetics Endocrinology Cardiovascular agent Adrenal Cortex cardiovascular system sense organs hormones hormone substitutes and hormone antagonists circulatory and respiratory physiology |
| Zdroj: | Biochemical and Biophysical Research Communications. 172:1195-1202 |
| ISSN: | 0006-291X |
| DOI: | 10.1016/0006-291x(90)91575-d |
| Popis: | [3H]DuP 753, a nonpeptide angiotensin II (AII) receptor antagonist radioligand, was used to characterize a subtype of AII receptors in rat adrenal cortical microsomes. By Scatchard analysis, a single class of DuP 753 binding sites was found with an affinity of 6.4 nM and a Bmax of 1.3 pmol/mg protein. These sites were saturable and readily reversible. Angiotensin (I, II, III) expressed the same affinities and order of potency for these binding sites as those labeled by [3H]AII for the AII-1 sites. The affinities expressed by nonpeptide AII antagonists were commensurate with their inhibitory potencies on AII-1 receptors. PD123177, an AII-2 specific ligand, and other non-AII peptides showed no inhibitory action. These data together with the differential tissue distribution strongly support our conclusion that [3H]DuP 753 is a potent and highly specific radioligand for the AII-1 receptors. |
| Databáze: | OpenAIRE |
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