| Autor: |
Provencher BA; Alcohol & Drug Abuse Research Center, ‡Mailman Research Center, McLean Hospital, Harvard Medical School , 115 Mill Street, Belmont, Massachusetts 02478, United States., Sromek AW, Li W, Russell S, Chartoff E, Knapp BI, Bidlack JM, Neumeyer JL |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2013 Nov 14; Vol. 56 (21), pp. 8872-8. Date of Electronic Publication: 2013 Oct 29. |
| DOI: |
10.1021/jm401290y |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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