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

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Blagg J, Allerton CM, Batchelor DV, Baxter AD, Burring DJ, Carr CL, Cook AS, Nichols CL, Phipps J, Sanderson VG, Verrier H, Wong S

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

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6691-6. Epub 2007 Oct 22.

PubMed ID
17976986 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ApomorphineDopamine D2 receptorEC 50 (nM)20N/AN/ADetails
ApomorphineDopamine D3 receptorEC 50 (nM)7N/AN/ADetails
RopiniroleDopamine D2 receptorEC 50 (nM)83N/AN/ADetails
RopiniroleDopamine D3 receptorEC 50 (nM)4N/AN/ADetails