Structure-activity relationships in a series of monocyclic endothelin analogues

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Abstract

Monocyclic fragment analogues of endothelin-1 (ET-1) were prepared to explore the importance of the bicyclic structure of ET-1 to its binding affinity and functional activity. Most of the monocyclic analogues prepared showed low micro to high nanomolar binding affinities and were functional antagonists of ET-1 induced accumulation of inositol phosphates. However, one analogue possessed mixed antagonist/agonist activity at the two endothelin receptor subtypes.

Monocylic fragment analogues of endothelin-1 (ET-1) were prepared to explore the importance of the bicyclic structure of ET-1 to its binding affinity and functional activity.

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