Antagonism of endothelin actions

Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Polymer from ethylenic monomers only

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424 92, 514 2, 514 12, A61K 4900, A61K 3800, G01N 3100, A61N 3117

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056884990

ABSTRACT:
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.

REFERENCES:
Banting et al., Increased endothelin activity plays a primary role hypertension induced by acute nitric oxide synthase blockade, FASEB Journal v.9 (3) p. A338, Mar. 9, 1995.
Wang et al., Involvement of endothelin-1 in hypoxic pulmonary vasoconstriction in the lamb, Journal of Physiology v.482 (2) pp. 421-434, Jan. 15, 1995.
Teerlink et al., Role of endothelin in the maintenance of blood pressure in concious rats with chronic heart failure, Circulation v.90 (5) pp. 2510-2518, Nov. 1994.
Luscher et al., Pharmacological inhibition of endothelin induced vasoconstriction in man: Focus on calcium channel blockers and endothelin receptor antagonists, Drugs of today v.31 (supple B) pp. 7-17, 1995.

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