Université De Sherbrooke

Gerard E Plante

Witold A Neugebauer

Fernand Gobeil

Adriana Zucollo

Orlando L Catanzaro

Domenico Recoli

The present invention relates to novel antagonists to a B-bradykinin (B-BK) receptor which have a good affinity and selectivity therefor, some of which being at least partially resistant to enzymatic degradation. The synthesis of the Breceptors is induced during inflammation. Symptoms associated with inflammation (elevated hydrostatic pressure and plasma leakage or extravasation) have been observed in diabetic animal models (streptozotocin-induced diabetes (STZ)) as well as in spontaneously hypertensive rats (SHR). The present inventors confirm the presence of B-BK receptors in these two models. B-BK antagonists abolished the vasocontraction induced by B-BK in SHR and STZ, and reduced the glycemia of diabetic animals to normal levels. The present B-antagonists are useful for treating any condition wherein B-receptor is expressed, particularly during inflammation, and more particularly wherein B-receptor expression results in diabetic vasculopathy, other diabetic symptoms associated with an insulitis and a post-capillary resistance building as a consequence of the presence of a B-receptor.

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Sherbrooke, Canada

Gerard E Plante