Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route

Bioorganic & Medicinal Chemistry Letters
2007.0

Abstract

This paper reports the synthesis and biological activity of a novel series of aryl-morpholine dopamine receptor agonists. Several compounds show high levels of functional selectivity for the D3 over the D2 dopamine receptor. Compound 26 has >1000-fold functional selectivity and has been successfully progressed in vivo using an intranasal delivery route.

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