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J Med Chem. 2013 Nov 14;56(21):8872-8. doi: 10.1021/jm401290y. Epub 2013 Oct 29.

Synthesis and pharmacological evaluation of aminothiazolomorphinans at the mu and kappa opioid receptors.

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Alcohol & Drug Abuse Research Center, ‡Mailman Research Center, McLean Hospital, Harvard Medical School , 115 Mill Street, Belmont, Massachusetts 02478, United States.


Previous studies with aminothiazolomorphinans suggested that this class of opioid ligands may be useful as a potential pharmacotherapeutic to decrease drug abuse. Novel aminothiazole derivatives of cyclorphan were prepared to evaluate a series of aminothiazolomorphinans with varying pharmacological properties at the κ opioid receptor (KOR) and μ opioid receptor (MOR). This study was focused on exploring the regioisomeric analogs with the aminothiazole on the C-ring of the morphinan skeleton. Receptor binding and [(35)S]GTPγS binding assays were used to characterize the affinity and pharmacological properties of the aminothiazolomorphinans. Intracranial self-stimulation (ICSS) was used to compare the effects of a representative aminothiazolomorphinan with the morphinan mixed-KOR/MOR agonist butorphan (MCL-101) on brain-stimulation reward.

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