In Vivo Pharmacology of Ro 46-2005, The First Synthetic Nonpeptide Endothelin Receptor Antagonist: Implications for Endothelin Physiology
- 1 January 1993
- journal article
- pathology
- Published by Wolters Kluwer Health in Journal of Cardiovascular Pharmacology
- Vol. 22 (Supplement) , S377-S379
- https://doi.org/10.1097/00005344-199322008-00099
Abstract
Summary: Ro 46-2005 is a small-molecular-weight nonpeptide antagonist of the endothelin (ET) ETA and ETB receptors, chemically derived from a class of compounds identified by systematic screening of chemicals. In vivo, Ro 46-2005 inhibited the depressor and, only at high doses (100 mg/kg i.v.) the pressor effect of ET-1. However, much lower doses (1 to 10 mg/kg i.v.) were sufficient to inhibit the pressor effect of the precursor big ET-1. As intravenous big ET-1 injection potentially reproduces better than ET-1 injection the physiological pattern of release of ET-1, we propose that intravenous big ET-1 should be used to evaluate the effects of antagonists on the constricting endothelin receptors.Keywords
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