Design, Synthesis, and Biological Evaluation of (3R)-1,2,3,4-Tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide (JDTic) Analogues: In Vitro Pharmacology and ADME Profile

[Image: see text] JDTic analogues 4–15 which have the hydroxyl groups replaced with other groups were synthesized and their in vitro efficacy at the μ, δ, and κ opioid receptors determined and compared to JDTic using [(35)S]GTPγS assays. Compounds 4, 5, 6, 13, 14, and 15 had K(e) = 0.024, 0.01, 0.03...

Descripción completa

Detalles Bibliográficos
Autores principales: Kormos, Chad M., Gichinga, Moses G., Maitra, Rangan, Runyon, Scott P., Thomas, James B., Brieaddy, Lawrence E., Mascarella, S. Wayne, Navarro, Hernán A., Carroll, F. Ivy
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4161151/
https://www.ncbi.nlm.nih.gov/pubmed/25133923
http://dx.doi.org/10.1021/jm5008177

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4161151/
https://www.ncbi.nlm.nih.gov/pubmed/25133923
http://dx.doi.org/10.1021/jm5008177

Ejemplares similares