In vitro characterization and comparison of JDTic, its dehydroxy analogue and nor-BNI, and its dehydroxy analogue demonstrates that the N-substituted 3,4-dimethyl-(3-hydroxyphenyl)-piperidine-derived antagonist, JDTic, relies more heavily on its phenol address group for affinity and antagonist activity relative to the corresponding naltrexone derived antagonists, nor-BNI. The structural flexibility of the former class of compound relative to the latter is postulated to underlie the difference
Importance of phenolic address groups in opioid kappa receptor selective antagonists
Thomas, J., Fix, S., Rothman, RB., Mascarella, S., Dersch, CM., Cantrell, BE., Zimmerman, DM., & Carroll, F. (2004). Importance of phenolic address groups in opioid kappa receptor selective antagonists. Journal of Medicinal Chemistry, 47(4), 1070-1073. https://doi.org/10.1021/jm030467v
Abstract
Publications Info
To contact an RTI author, request a report, or for additional information about publications by our experts, send us your request.
Meet the Experts
View All ExpertsRecent Publications
Article
Rate of onset of dopamine transporter inhibitors assessed with intracranial self-stimulation and in vivo dopamine photometry in rats
OCCASIONAL PAPER
Equipping health professions educators to better address medical misinformation
Article
Molecular mechanism of biased signaling at the kappa opioid receptor
Article