Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor.

Tran, Joe A; Chen, Caroline W; Jiang, Wanlong; Tucci, Fabio C; Fleck, Beth A; Marinkovic, Dragan; Arellano, Melissa; Chen, Chen

Tran, Joe A; Chen, Caroline W; Jiang, Wanlong; Tucci, Fabio C; Fleck, Beth A; Marinkovic, Dragan; Arellano, Melissa; Chen, Chen.

Afiliação

Tran JA; Department of Medicinal Chemistry, Neurocrine Biosciences, Inc., 12790 El Camino Real, San Diego, CA 92130, USA.

Bioorg Med Chem Lett ; 17(18): 5165-70, 2007 Sep 15.

Article em En | MEDLINE | ID: mdl-17629702

ABSTRACT

ABSTRACT

A series of pyrrolidine derivatives were synthesized and characterized as potent agonists of the human melanocortin-4 receptor. For example, 28c had a K(i) of 13 nM in binding affinity and EC(50) of 6.9 nM in agonist potency with an intrinsic activity of 100% of the endogenous ligand alpha-MSH.

Assuntos

Pirrolidinas/farmacologia; Receptor Tipo 4 de Melanocortina/agonistas; Linhagem Celular; Humanos

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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirrolidinas / Receptor Tipo 4 de Melanocortina Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2007 Tipo de documento: Article País de afiliação: Estados Unidos

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