Vasodilator effects of the endothelin ETA receptor selective antagonist BMS-193884 in healthy men
| Autor: | Neville F. Ford, Neil R. Johnston, Neeraj Dhaun, David J. Webb, Maria Palmisano, David E. Newby, Janis L. Hammett, Fiona E. Strachan |
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| Rok vydání: | 2005 |
| Předmět: |
Pharmacology
medicine.medical_specialty business.industry Hemodynamics Vasodilation Endothelin 1 Endothelin A Receptor Antagonists stomatognathic diseases medicine.anatomical_structure Endocrinology Oral administration Internal medicine Vascular resistance medicine Pharmacology (medical) medicine.symptom Endothelin receptor business Vasoconstriction |
| Zdroj: | British Journal of Clinical Pharmacology. 60:611-622 |
| ISSN: | 0306-5251 |
| Popis: | Aims A number of endothelin receptor antagonists (ERAs) are currently in clinical development as potential therapies in states characterized by vasoconstriction, such as systemic hypertension. We investigated the haemodynamic effects of locally and systemically active doses of BMS-193884, an endothelin A (ETA) receptor selective ERA, and its influence on vasoconstriction to endothelin-1 (ET-1) in healthy men. Methods In three separate randomized, placebo-controlled studies, the forearm blood flow (FBF) response to intra-arterial (i.a.) infusion of ET-1 (5 pmol min−1) was assessed during i.a. co-infusion of BMS-193884 (5 and 50 nmol min−1), and at 12 and at 24 h after oral administration of BMS-193884 (50, 100 and 200 mg at 12 h; and 200 mg at 24 h). Data were examined by repeated-measures analysis of variance (anova) with treatment and subject as factors. Results ET-1 caused significant forearm vasoconstriction, attenuated after oral dosing with BMS-193884 (200 mg) at 12 (P |
| Databáze: | OpenAIRE |
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