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]
- 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
Drug Target Property Measurement pH Temperature (°C) Apomorphine Dopamine D2 receptor EC 50 (nM) 20 N/A N/A Details Apomorphine Dopamine D3 receptor EC 50 (nM) 7 N/A N/A Details Ropinirole Dopamine D2 receptor EC 50 (nM) 83 N/A N/A Details Ropinirole Dopamine D3 receptor EC 50 (nM) 4 N/A N/A Details