Discovery of an Opioid κ Receptor Selective Pure Antagonist from a Library of N-Substituted 4β-Methyl-5-(3-hydroxyphenyl)morphans
Journal of Medicinal Chemistry2002Vol. 45(16), pp. 3524–3530
Citations Over Time
James B. Thomas, Robert N. Atkinson, Nivedita Namdev, Richard B. Rothman, Kenneth M. Gigstad, Scott E. Fix, S. Wayne Mascarella, Jason P. Burgess, N. Ariane Vinson, Heng Xu, Christina M. Dersch, Buddy E. Cantrell, Dennis M. Zimmerman, F. Ivy Carroll
Abstract
A library of compounds biased toward opioid receptor antagonist activity was prepared by incorporating N-phenylpropyl-4beta-methyl-5-(3-hydroxyphenyl)morphans as the core scaffold using simultaneous solution phase synthetic methodology. From this library, N-phenylpropyl-4beta-methyl-5-(3-hydroxyphenyl)-7alpha-[3-(1-piperidinyl)propanamido]morphan [(-)-3b] was identified as the first potent and selective kappa opioid receptor antagonist from the 5-phenylmorphan class of opioids.
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