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Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.
Blagg J,
Allerton CM,
Batchelor DV,
Baxter AD,
Burring DJ,
Carr CL,
Cook AS,
Nichols CL,
Phipps J,
Sanderson VG,
Verrier H,
Wong S.
Pfizer Global Research & Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
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.
PMID: 17976986 [PubMed - indexed for MEDLINE]
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