1. Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route
- Author
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Denise J. Burring, Carly L. Nichols, Vivienne Sanderson, David V. Batchelor, Charlotte Moira Norfor Allerton, Andrew Simon Cook, Julian Blagg, Joanne Phipps, Hugh Verrier, Stephen K.-F. Wong, Andrew Douglas Baxter, and Christopher L. Carr
- Subjects
Models, Molecular ,Agonist ,medicine.drug_class ,Clinical Biochemistry ,Pharmaceutical Science ,Pharmacology ,Crystallography, X-Ray ,Biochemistry ,Structure-Activity Relationship ,Dogs ,In vivo ,Dopamine receptor D3 ,Drug Discovery ,Functional selectivity ,medicine ,Animals ,Humans ,Structure–activity relationship ,Receptor ,Molecular Biology ,Administration, Intranasal ,Molecular Structure ,Chemistry ,Organic Chemistry ,Receptors, Dopamine D3 ,Stereoisomerism ,Biological activity ,Rats ,Dopamine receptor ,Drug Design ,Dopamine Agonists ,Molecular Medicine - 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.
- Published
- 2007
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