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

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

Affiliation

  • 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.

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