Binding kinetics of budesonide to the human glucocorticoid receptor
| Autor: | Peter Rohdewald, N Esmailpour, Petra Högger |
|---|---|
| Rok vydání: | 1998 |
| Předmět: |
Budesonide
medicine.medical_specialty Chemistry Pharmaceutical Science Dexamethasone Receptor–ligand kinetics Fluticasone propionate Dissociation constant Receptors Glucocorticoid Glucocorticoid receptor Endocrinology Internal medicine medicine Humans Receptor Glucocorticoid medicine.drug Fluticasone |
| Zdroj: | European Journal of Pharmaceutical Sciences. 6:219-223 |
| ISSN: | 0928-0987 |
| Popis: | Glucocorticoid receptor-ligand binding kinetics of budesonide, a glucocorticoid used for inhalation therapy, were determined and compared with dexamethasone and fluticasone propionate using glucocorticoid receptors from human lung tissue. From the association constant of 18.9 x 10(5)l mol-1 min-1 and the dissociation constant of 25.0 x 10(-4) min-1 resulted the equilibrium dissociation constant KD of 1.32 nmol/l and a relative receptor affinity of 855 with dexamethasone as reference (100). The half-life of the budesonide-receptor complex was 4.6 h. Results agree with data derived from competition tests we performed earlier. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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