Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists

Fabrizio Micheli; Susanna Cremonesi; Teresa Semeraro; Luca Tarsi; Silvia Tomelleri; Paolo Cavanni; Beatrice Oliosi; Elisabetta Perdonà; Anna Sava; Laura Zonzini; Aldo Feriani; Simone Braggio; Christian Heidbreder

doi:10.1016/j.bmcl.2015.12.081

Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1329-32. doi: 10.1016/j.bmcl.2015.12.081. Epub 2016 Jan 5.

Affiliations

¹ Aptuit s.r.l, Via Fleming 4, 37135 Verona, Italy.
² Indivior Inc, The Fairfax Building, 10710 Midlothian Turnpike, Suite 430, Richmond, VA 23235, USA.

PMID: 26786693
DOI: 10.1016/j.bmcl.2015.12.081

Abstract

A new series of morpholine derivatives has been identified as selective DA D3 receptor antagonists; their in vitro profile and pharmacokinetic data are provided.

Keywords: 7-TM; Antagonist; DA D3 receptor; Dopamine; Morpholine.

MeSH terms

Animals
Binding Sites
Dopamine D2 Receptor Antagonists / chemical synthesis
Dopamine D2 Receptor Antagonists / chemistry*
Dopamine D2 Receptor Antagonists / pharmacokinetics
Half-Life
Molecular Docking Simulation
Morpholines / chemical synthesis
Morpholines / chemistry*
Morpholines / pharmacokinetics
Protein Structure, Tertiary
Rats
Receptors, Dopamine D3 / antagonists & inhibitors*
Receptors, Dopamine D3 / metabolism

Substances

Dopamine D2 Receptor Antagonists
Morpholines
Receptors, Dopamine D3
morpholine