Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists.
J Med Chem
; 50(20): 4789-92, 2007 Oct 04.
Article
em En
| MEDLINE
| ID: mdl-17850061
ABSTRACT
A 1,3,4-benzotriazepine was identified as a suitable lead in our effort toward obtaining a non-peptide parathyroid hormone-1 receptor (PTH1R) antagonist. A process of optimization afforded derivatives displaying nanomolar PTH1R affinity, a representative example of which behaved as a PTH1R antagonist in cell-based cyclic adenosine monophosphate (cAMP) assays, with selectivity over PTH2 receptors.
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Base de dados:
MEDLINE
Assunto principal:
Benzazepinas
/
Receptor Tipo 1 de Hormônio Paratireóideo
Limite:
Animals
/
Humans
Idioma:
En
Revista:
J Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2007
Tipo de documento:
Article
País de afiliação:
Reino Unido