Phenylethynyl-pyrrolo[1,2-a]pyrazine: A new potent and selective tool in the mGluR5 antagonists arena

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 6, 2008, Pages 1804-1809

  Micheli, Fabrizio ^a   Bertani, Barbara ^a   Bozzoli, Andrea ^a   Crippa, Luca ^a   Cavanni, Paolo ^a   Di Fabio, Romano ^a   Donati, Daniele ^a   Marzorati, Paola ^a   Merlo, Giancarlo ^a   Paio, Alfredo ^a   Perugini, Lorenzo ^a   Zarantonello, Paola ^a  

^a GSK   (Italy)

Author keywords

7 TM; Antagonists; Metabotropic; mGluR5; Receptor

Indexed keywords

GLUTAMATE RECEPTOR 5; GLUTAMATE RECEPTOR 5 BLOCKING AGENT; GLUTAMATE RECEPTOR ANTAGONIST; PHENYLETHYNYLPYRROLO[1,2 A]PYRAZINE; UNCLASSIFIED DRUG;

ARTICLE; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; IC 50; RECEPTOR BLOCKING; STRUCTURE ACTIVITY RELATION;

DOPAMINE PLASMA MEMBRANE TRANSPORT PROTEINS; FLUORESCENCE; HUMANS; MOLECULAR STRUCTURE; NOREPINEPHRINE PLASMA MEMBRANE TRANSPORT PROTEINS; PYRAZINES; PYRROLES; RECEPTORS, METABOTROPIC GLUTAMATE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 40849123742     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.02.024     Document Type: Article

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19. Activity is measured as the alteration of a glutamate induced increase in intracellular calcium which activates a fluorescent dye loaded into the cells. The fluorescence produced is measured by FLIPR™. Chinese Hamster Ovary cells transfected with the h-mGluR5 receptor under the control of the GeneSwitch™ Gene Expression apparatus were used.
20. 3 at room temperature for 20 h, followed by appropriate chromatographic separation (CyH-AcOEt from 90/10 to 80/20).