[Endothelin-1 and cardiovascular diseases].
BACKGROUND
Endothelins are peptides released from endothelial cells. According to both their structure and receptor affinity, three isoforms may be identified. Endothelin-1 is secreted abluminally by endothelial cells, and binds ETA and ETB2 receptors expressed on vascular smooth muscle cells, and ETB1 expressed on endothelial cells. ETA and ETB2 receptors stimulation induces smooth muscle contraction and proliferation, whereas ETB1 receptors stimulation induces relaxation.


BACKGROUND
Endothelin-1 plays an important role in maintaining peripheral vascular tone and systemic blood pressure. It is recognized to have a role in various diseases associated with vasoconstriction and vascular hypertrophy.


CONCLUSIONS
Recent development of endothelin receptor antagonists seems promising for the treatment of heart failure and systemic hypertension, with interesting results obtained from short-term clinical trials. However, better evaluation of these drugs requires further long-term studies regarding not only the above mentioned diseases but also ischemic heart disease or pulmonary hypertension. Endothelin antagonists are therefore new therapeutic agents able to inhibit a vasoconstricting system that has been recently discovered. Results of ongoing clinical studies are awaited with interest.
Cracowski
J L
JL
Laboratoire de pharmacologie, PCEBM, faculté de médecine, La Tronche, France.
Stanke
F
F
Bessard
G
G
D002318:Cardiovascular Diseases / Q000188:drug therapy / Q000503:physiopathology*; D002986:Clinical Trials as Topic; D065128:Endothelin Receptor Antagonists; D019332:Endothelin-1 / Q000502:physiology*; D006801:Humans; D009131:Muscle, Smooth, Vascular / Q000502:physiology* / Q000503:physiopathology; D044022:Receptor, Endothelin A; D044023:Receptor, Endothelin B; D017466:Receptors, Endothelin / Q000502:physiology*
D065128:Endothelin Receptor Antagonists; D019332:Endothelin-1; D044022:Receptor, Endothelin A; D044023:Receptor, Endothelin B; D017466:Receptors, Endothelin
Endothéline-1 et pathologies cardiovasculaires.