Novel Phenyl-Substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 Antagonists with Robust Target Engagement in Rat Brain.

Chrovian, Christa C; Soyode-Johnson, Akinola; Ao, Hong; Bacani, Genesis M; Carruthers, Nicholas I; Lord, Brian; Nguyen, Leslie; Rech, Jason C; Wang, Qi; Bhattacharya, Anindya; Letavic, Michael A

Chrovian, Christa C; Soyode-Johnson, Akinola; Ao, Hong; Bacani, Genesis M; Carruthers, Nicholas I; Lord, Brian; Nguyen, Leslie; Rech, Jason C; Wang, Qi; Bhattacharya, Anindya; Letavic, Michael A.

Afiliação

Chrovian CC; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.
Soyode-Johnson A; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.
Ao H; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.
Bacani GM; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.
Carruthers NI; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.
Lord B; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.
Nguyen L; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.
Rech JC; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.
Wang Q; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.
Bhattacharya A; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.
Letavic MA; Janssen Research & Development, LLC , 3210 Merryfield Row, San Diego, California 92121-1126, United States.

ACS Chem Neurosci ; 7(4): 490-7, 2016 Apr 20.

Article em En | MEDLINE | ID: mdl-26752113

Assuntos

Encéfalo/efeitos dos fármacos; Antagonistas do Receptor Purinérgico P2X/química; Antagonistas do Receptor Purinérgico P2X/farmacologia; Pirazinas/química; Pirazinas/farmacologia; Animais; Autorradiografia; Ligação Competitiva/efeitos dos fármacos; Relação Dose-Resposta a Droga; Humanos; Técnicas In Vitro; Concentração Inibidora 50; Ligação Proteica/efeitos dos fármacos; Ratos; Relação Estrutura-Atividade

Palavras-chave

P2X7; SAR; brain permeability; mood disorders; receptor occupancy

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Limite: Animals / Humans Idioma: En Ano de publicação: 2016 Tipo de documento: Article

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Limite: Animals / Humans Idioma: En Ano de publicação: 2016 Tipo de documento: Article