1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists

[Display omitted] A novel series of 1,2,4-triazolyl octahydropyrrolo[2,3-b]pyrroles showing high affinity and selectivity at the DA D3 receptor is reported here. Compounds endowed with high selectivity over the hERG channel were identified and their pharmacokinetic properties thoroughly analyzed. A...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2016-04, Vol.24 (8), p.1619-1636
Hauptverfasser:	Micheli, Fabrizio, Bernardelli, Andrea, Bianchi, Federica, Braggio, Simone, Castelletti, Laura, Cavallini, Palmina, Cavanni, Paolo, Cremonesi, Susanna, Cin, Michele Dal, Feriani, Aldo, Oliosi, Beatrice, Semeraro, Teresa, Tarsi, Luca, Tomelleri, Silvia, Wong, Andrea, Visentini, Filippo, Zonzini, Laura, Heidbreder, Christian
Format:	Artikel
Sprache:	eng
Schlagworte:	Addiction Animals Antagonist Binding, Competitive - drug effects CHO Cells Cricetulus DA D3 receptor Dopamine Dose-Response Relationship, Drug Ether-A-Go-Go Potassium Channels - antagonists & inhibitors HEK293 Cells Humans Models, Molecular Molecular Structure Neuroscience Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - pharmacology Receptors, Dopamine D3 - antagonists & inhibitors Structure-Activity Relationship Triazoles - chemical synthesis Triazoles - chemistry Triazoles - pharmacology
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