Structure-activity relationship of the cholestatic activity of dihydrotestosterone glucuronide, allo bile acids and lithocholate
| Autor: | Sherrie Durham, Schlarman D, Christopher L. Montgomery, Mary Vore, Elliott Wh |
|---|---|
| Rok vydání: | 1989 |
| Předmět: |
medicine.medical_specialty
medicine.drug_class medicine.medical_treatment General Biochemistry Genetics and Molecular Biology Steroid Bile Acids and Salts chemistry.chemical_compound Structure-Activity Relationship Trans configuration Internal medicine medicine Structure–activity relationship Dihydrotestosterone glucuronide Moiety Potency Animals Bile General Pharmacology Toxicology and Pharmaceutics Bile acid Dose-Response Relationship Drug Molecular Structure Dihydrotestosterone Rats Inbred Strains General Medicine Glucuronic acid Rats Endocrinology chemistry Female Lithocholic Acid Secretory Rate |
| Zdroj: | Life sciences. 44(26) |
| ISSN: | 0024-3205 |
| Popis: | Dihydrotestosterone glucuronide (DHTG), a series of 5 alpha-bile acids, or allo-bile acids (3 alpha-hydroxy-5 alpha-cholanic acid, 3-keto-5 alpha-cholanic acid and 3 beta-hydroxy-5 alpha-cholanic acid) and their normal bile acid analogues (3 alpha-hydroxy-5 beta-cholanic acid or lithocholate, 3-keto-5 beta-cholanic acid and 3 beta-hydroxy-5 beta-cholanic acid) were administered intravenously to female rats in order to determine their effects on bile flow. All agents caused a rapid and profound inhibition of bile flow which was dose-dependent. The logarithm of the dose vs the cholestatic response curve for DHTG, the allo-bile acids and lithocholate were all parallel. DHTG was the most potent congener and was two times more potent than 3-keto-5 alpha-cholanic acid and 5 times more potent than lithocholate. These data indicate that the glucuronic acid moiety and the trans configuration of the A and B rings of the steroid nucleus confer the greatest cholestatic potency. |
| Databáze: | OpenAIRE |
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