Highly potent and selective phenylmorphan-based inverse agonists of the opioid δ receptor

JB Thomas, L Zhang, HA Navarro…

文献索引：Carroll, F. Ivy; Melvin, Matt S.; Nuckols, Michel C.; Mascarella, S. Wayne; Navarro, Hernan A.; Thomas, James B. Journal of Medicinal Chemistry, 2006 , vol. 49, # 5 p. 1781 - 1791

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被引用次数: 13

摘要

We recently reported the discovery of (+)-5-(3-hydroxyphenyl)-4-methyl-2-(3-phenylpropyl)-2- azabicyclo [3.3. 1] non-7-yl-(1-phenyl-1-cyclopentane) carboxamide [(+)-KF4,(+)-5] as a novel chemotype possessing potent antagonist activity at the δ opioid receptor. Additional SAR studies involving changes to both the 2-amino and 7-amido N-substituents using this same (+)-morphan scaffold have revealed compounds with improved potency and ...