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Studies toward bivalent κ opioids derived from salvinorin A: heteromethylation of the furan ring reduces affinity

The recent crystal structure of the κ-opioid receptor (κ-OR) revealed, unexpectedly, that the antagonist JDTic is a bivalent ligand: in addition to the orthosteric pocket occupied by morphinans, JDTic also occupies a distinct (allotopic) pocket. Mutagenesis data suggest that salvinorin A (1) also bi...

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Detalles Bibliográficos
Autores principales: Munro, Thomas A, Xu, Wei, Ho, Douglas M, Liu-Chen, Lee-Yuan, Cohen, Bruce M
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Beilstein-Institut 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3896271/
https://www.ncbi.nlm.nih.gov/pubmed/24454571
http://dx.doi.org/10.3762/bjoc.9.328