| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376035 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
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.
Graphical abstractSynthesis and dopamine receptor agonist activity of a novel series of aryl-morpholines is disclosed. Compound 26 shows high functional in vitro selectivity for activation the dopamine D3 receptor. In vivo properties of this compound are also reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Julian Blagg, Charlotte M.N. Allerton, David V.J. Batchelor, Andrew D. Baxter, Denise J. Burring, Christopher L. Carr, Andrew S. Cook, Carly L. Nichols, Joanne Phipps, Vivienne G. Sanderson, Hugh Verrier, Stephen Wong,