Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.

Basic Information

ID: ALA1135969

Journal: J Med Chem

Title: Discovery of an opioid kappa receptor selective pure antagonist from a library of N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphans.

Authors: Thomas JB, Atkinson RN, Namdev N, Rothman RB, Gigstad KM, Fix SE, Mascarella SW, Burgess JP, Vinson NA, Xu H, Dersch CM, Cantrell BE, Zimmerman DM, Carroll FI.

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.

CiteXplore: 12139463

DOI: 10.1021/jm020084h

Patent ID: ┄