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Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif

dc.contributor.authorFrankowski, Kevin J.
dc.contributor.authorSlauson, Stephen R.
dc.contributor.authorMovell, Kimberly M.
dc.contributor.authorPhillips, Angela M.
dc.contributor.authorStreicher, John M.
dc.contributor.authorZhou, Lei
dc.contributor.authorWhipple, David A.
dc.contributor.authorSchoenen, Frank J.
dc.contributor.authorPrisinzano, Thomas E.
dc.contributor.authorBohn, Laura M.
dc.contributor.authorAubé, Jeffrey
dc.date.accessioned2017-05-10T18:26:15Z
dc.date.available2017-05-10T18:26:15Z
dc.date.issued2015-07-15
dc.identifier.citationFrankowski, K. J., Slauson, S. R., Lovell, K. M., Phillips, A. M., Streicher, J. M., Zhou, L., … Aubé, J. (2015). Potency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motif. Bioorganic & Medicinal Chemistry, 23(14), 3948–3956. http://doi.org/10.1016/j.bmc.2014.12.033en_US
dc.identifier.urihttp://hdl.handle.net/1808/24079
dc.description.abstractOptimization of the sulfonamide-based kappa opioid receptor (KOR) antagonist probe molecule ML140 through constraint of the sulfonamide nitrogen within a tetrahydroisoquinoline moiety afforded a marked increase in potency. This strategy, when combined with additional structure-activity relationship exploration, has led to a compound only six-fold less potent than norBNI, a widely utilized KOR antagonist tool compound, but significantly more synthetically accessible. The new optimized probe is suitably potent for use as an in vivo tool to investigate the therapeutic potential of KOR antagonists.en_US
dc.publisherElsevieren_US
dc.rightsThis article is made available under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0) License.en_US
dc.rights.urihttps://creativecommons.org/licenses/by-nc-nd/3.0/en_US
dc.subjectKappa Opioid Receptoren_US
dc.subjectAntagonisten_US
dc.subjectMolecular constrainten_US
dc.subjectPotency enhancementen_US
dc.subjectTetrahydroisoquinolineen_US
dc.titlePotency enhancement of the κ-opioid receptor antagonist probe ML140 through sulfonamide constraint utilizing a tetrahydroisoquinoline motifen_US
dc.typeArticleen_US
kusw.kuauthorFrankowski, Kevin J.
kusw.kuauthorSlauson, Stephen R.
kusw.kuauthorWhipple, David A.
kusw.kuauthorSchoenen, Frank J.
kusw.kuauthorPrisinzano, Thomas E.
kusw.kuauthorAubé, Jeffrey
kusw.kudepartmentSpecialized Chemistry Centeren_US
kusw.oanotesPer SherpaRomeo on 05/10/2017: Author's Pre-print: green tick author can archive pre-print (ie pre-refereeing) Author's Post-print: green tick author can archive post-print (ie final draft post-refereeing) Publisher's Version/PDF: cross author cannot archive publisher's version/PDF General Conditions: Authors pre-print on any website, including arXiv and RePEC Author's post-print on author's personal website immediately Author's post-print on open access repository after an embargo period of between 12 months and 48 months Permitted deposit due to Funding Body, Institutional and Governmental policy or mandate, may be required to comply with embargo periods of 12 months to 48 months Author's post-print may be used to update arXiv and RepEC Publisher's version/PDF cannot be used Must link to publisher version with DOI Author's post-print must be released with a Creative Commons Attribution Non-Commercial No Derivatives Licenseen_US
dc.identifier.doi10.1016/j.bmc.2014.12.033en_US
dc.identifier.orcidhttps://orcid.org/0000-0003-1049-5767 https://orcid.org/0000-0002-2811-2894
kusw.oaversionScholarly/refereed, author accepted manuscripten_US
kusw.oapolicyThis item meets KU Open Access policy criteria.en_US
dc.identifier.pmidPMC4468036en_US
dc.rights.accessrightsopenAccess


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This article is made available under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0) License.
Except where otherwise noted, this item's license is described as: This article is made available under a Creative Commons Attribution-NonCommercial-NoDerivs 3.0 Unported (CC BY-NC-ND 3.0) License.