Antagonism of endothelin actions

Details Antagonism of endothelin actions Antagonism of endothelin actions

A - Human Necessities

61

K

A61K 38/18 (2006.01) A61K 31/505 (2006.01) A61K 31/70 (2006.01) A61K 38/06 (2006.01) A61K 38/10 (2006.01) A61K 38/12 (2006.01) A61K 38/14 (2006.01) A61K 38/22 (2006.01) A61K 48/00 (2006.01)

Patent

CA 2248047

The mechanism of hypertension following acute NO synthase blockade is via endothelin-mediated vasoconstriction. Thus, NO appears to inhibit endothelin activity by blocking its expression and not as a chronic direct acting vasodilator. Administration of an endothelin antagonist to a patient in a 'normal' physiological state may result in specific regional vasodilation. This treatment finds utility in the treatment of erectile dysfunction.

Le mécanisme d'hypertension qui suit le blocage aigu de la NO synthase se traduit par une vasoconstriction induite par l'endothéline. Donc, NO semble inhiber l'activité de l'endothéline par le blocage de son expression et non par l'action directe d'un vasodilatateur chronique. L'administration d'un antagoniste de l'entodhéline à un patient présentant un état physiologique "normal" peut entraîner une vasodilatation régionale spécifique. Ce traitement s'avère être utile pour traiter la dysérection.

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