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Title:

Human native kappa opioid receptor functions not predicted by recombinant receptors: {Implications} for drug design.

Document type:
Zeitschriftenaufsatz
Author(s):
Broad, John; Maurel, Damien; Kung, Victor W. S.; Hicks, Gareth A.; Schemann, Michael; Barnes, Michael R.; Kenakin, Terrence P.; Granier, Sebastien; Sanger, Gareth J.
Abstract:
If activation of recombinant G protein-coupled receptors in host cells (by drugs or other ligands) has predictive value, similar data must be obtained with native receptors naturally expressed in tissues. Using mouse and human recombinant kappa opioid receptors transfected into a host cell, two selectively-acting compounds (ICI204448, asimadoline) equi-effectively activated both receptors, assessed by measuring two different cell signalling pathways which were equally affected without evidence...     »
Journal title:
Scientific reports
Year:
2016
Journal volume:
6
Month:
aug
Pages contribution:
30797
Language:
eng
Fulltext / DOI:
doi:10.1038/srep30797
Print-ISSN:
2045-2322 2045-2322
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