Ex vivo inhibition of β-thromboglobulin release following administration to man of ABT-299, a novel prodrug of a potent platelet activating factor antagonist
| Autor: | H. D. Kleinert, T. J. Magoc, George W. Carter, Douglas W. Morgan, S. D. Menacherry, James B. Summers, E. Sun, A. E. Reyes, Daniel H. Albert |
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| Rok vydání: | 1997 |
| Předmět: |
Adult
Male Indoles Adolescent Metabolite Immunology Pyridinium Compounds In Vitro Techniques Pharmacology chemistry.chemical_compound Double-Blind Method Humans Prodrugs Platelet activation Platelet Activating Factor Chromatography High Pressure Liquid Dose-Response Relationship Drug Platelet-activating factor Chemistry Antagonist Prodrug beta-Thromboglobulin Thiazoles Beta-thromboglobulin Injections Intravenous Platelet aggregation inhibitor Platelet Aggregation Inhibitors Ex vivo |
| Zdroj: | Inflammation Research. 46:272-277 |
| ISSN: | 1420-908X 1023-3830 |
| Popis: | Objective and Design: ABT-299 is a prodrug that is converted by serum esterase to a potent platelet activating factor (PAF) antagonist (A-85783). In order to evaluate the pharmacological activity of this antagonist in man the effect of ABT-299 given to healthy volunteers on ex vivo PAF-induced β-thromboglobulin (β-TG) release in blood was assessed.¶Subjects: 37 healthy male volunteers, age 18 to 40 (mean age of 23.6 years) and free of medication, participated in the study.¶Treatment: Subjects were administered intravenously 0.8 mg, 2 mg, or 70 mg doses of ABT-299 (6–7 subjects per group) or placebo (9 subjects, pooled).¶Methods: Peripheral blood taken over 12 h after dosing was used for ex vivo β-TG release and, in the case of the 70 mg dose, measurement of plasma drug concentration. Data were compared by Student's t-test.¶Results: All three doses produced highly significant inhibition (p |
| Databáze: | OpenAIRE |
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