Endothelin and its inhibitors
Bruno Battistini,Timothy D. Warner +1 more
- 01 Jan 2001
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TL;DR: Endothelin Ligands and Their Experimental Effects Within the Human Circulation and the Roles of Endothelins in Proliferation, Apoptosis and Angiogenesis are explained.
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Abstract: 1. Historical Perspective and Introduction.- 2. Sarafotoxins.- 3. Endothelin-Converting Enzymes.- 4. Endothelin Receptors.- 5. Cell Signalling by Endothelin Peptides.- 6. Gene Deletion of Endothelin Systems.- 7. Endothelin-Converting Enzyme Inhibitors.- 8. Endothelin-Converting Enzymes and Endothelin Receptor Localisation in Human Tissues.- 9. Endothelin Receptor Antagonists.- 10. Toxicology of Endothelin Antagonists.- 11. Release of Autacoids.- 12. The Roles of Endothelins in Proliferation, Apoptosis and Angiogenesis.- 13. Endothelins in Cerebral Vasospasms and Strokes.- 14. Airway Reactivity and Disease.- 15. Endothelin-1 and Pulmonary Hypertension.- 16. Vascular and Cardiac Effects.- 17. Liver and Gastrointestinal System.- 18. Endothelins and the Kidney.- 19. Endothelin Ligands and Their Experimental Effects Within the Human Circulation.The complete table of contents can be found on the Internet: http://www.springer.de
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Characterization and localization of endothelin receptor subtypes in the human atrioventricular conducting system and myocardium
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39
References
ETA receptor-mediated constrictor responses to endothelin peptides in human blood vessels in vitro.
TL;DR: It is shown that in human isolated blood vessels, ET‐1 is more potent than ET‐3 suggesting the presence of vasoconstrictor ETA receptors.
148
Cerebral microvessel endothelium is producing endothelin.
Satonobu Yoshimoto,Yasuki Ishizaki,Hiroki Kurihara,Tomio Sasaki,Masao Yoshizumi,Masashi Yanagisawa,Yoshio Yazaki,Tomoh Masaki,Kintomo Takakura,Sei-itsu Murota +9 more
TL;DR: The results raise the possibility that the endothelia of cerebral microvessels regulate the local blood flow within the brain through the production of endothelin, a potent vasoconstrictor peptide.
148
Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.
Riechers Hartmut,Hans-Peter Albrecht,Willi Amberg,Ernst Dr. Baumann,Harald Dr. Bernard,Hans-Joachim Bohm,Klinge Dagmar,Andreas Kling,Stefan Müller,Manfred Raschack,Liliane Unger,Nigel Walker,Wolfgang Wernet +12 more
TL;DR: A novel class of endothelin-A receptor ligands was discovered by high-throughput screening which can be synthesized in a short sequence and show a long duration of action.
147
Putative precursors of endothelin have less vasoconstrictor activity in vitro but a potent pressor effect in vivo.
Tomoko Kashiwabara,Yoshimasa Inagaki,Hideo Ohta,Akihiro Iwamatsu,Motoyoshi Nomizu,Akihito Morita,Koji Nishikori +6 more
TL;DR: Endothelin (ET‐21) induced a sustained contraction of rat thoracic aortae in vitro, and caused a potent pressor effect in vivo after intravenous administration to rats, and the precursor deduced from porcine cDNA coding ET‐21 (pET‐39) had 100‐fold less contractile activity in vitro and in vivo.
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