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. doi: 10.1016/j.bmcl.2007.10.059.
Julian Blagg  1 ,  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
Affiliations
  • 1. Pfizer Global Research & Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
PMID: 17976986 DOI: 10.1016/j.bmcl.2007.10.059
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.