Synthesis and pharmacological characterization of two novel, brain penetrating P2X7 antagonists

ACS Medicinal Chemistry Letters

Volumn 4, Issue 4, 2013, Pages 419-422

  Letavic, Michael A ^a   Lord, Brian ^a   Bischoff, Francois ^a   Hawryluk, Natalie A ^a   Pieters, Serge ^a   Rech, Jason C ^a   Sales, Zachary ^a   Velter, Adriana I ^a   Ao, Hong ^a   Bonaventure, Pascal ^a   Contreras, Victor ^a   Jiang, Xiaohui ^a   Morton, Kirsten L ^a   Scott, Brian ^a   Wang, Qi ^a   Wickenden, Alan D ^a   Carruthers, Nicholas I ^a   Bhattacharya, Anindya ^a  

^a JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

depression; neuro inflammation; P2X7

Indexed keywords

2 METHYL N [[1 (4 PHENYLPIPERAZIN 1 YL)CYCLOHEXYL]METHYL] 1,2,3,4 TETRAHYDROISOQUINOLINE 5 CARBOXAMIDE; AMIDE; IMIDAZOLIDINECARBOXAMIDE; INTERLEUKIN 1BETA; N [[4 (4 PHENYL PIPERAZIN 1 YL)TETRAHYDRO 2H PYRAN 4 YL] METHYL] 2 (PHENYL THIO) NICOTINAMIDE; PURINERGIC P2X RECEPTOR ANTAGONIST; PURINERGIC P2X7 RECEPTOR ANTAGONIST; PYROGLUTAMIC ACID DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; AUTORADIOGRAPHY; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG BRAIN LEVEL; DRUG PENETRATION; DRUG SOLUBILITY; DRUG SYNTHESIS; EX VIVO STUDY; GLIA CELL; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; MOLECULE; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; RAT; RECEPTOR BLOCKING; RECEPTOR OCCUPANCY; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALIA; RATTUS;

EID: 84876263632     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/ml400040v     Document Type: Article

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