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Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.
Blagg, Julian; Allerton, Charlotte M N; Batchelor, David V J; Baxter, Andrew D; Burring, Denise J; Carr, Christopher L; Cook, Andrew S; Nichols, Carly L; Phipps, Joanne; Sanderson, Vivienne G; Verrier, Hugh; Wong, Stephen.
Bioorg Med Chem Lett ; 17(24): 6691-6, 2007 Dec 15.
Article in English | MEDLINE | ID: mdl-17976986

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.


Subject(s)
Dopamine Agonists/administration & dosage , Dopamine Agonists/chemical synthesis , Drug Design , Receptors, Dopamine D3/agonists , Administration, Intranasal , Animals , Crystallography, X-Ray , Dogs , Dopamine Agonists/chemistry , Dopamine Agonists/pharmacokinetics , Humans , Models, Molecular , Molecular Structure , Rats , Receptors, Dopamine D3/metabolism , Stereoisomerism , Structure-Activity Relationship
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