| Autor: |
Carroll, F. I., Zhang, L., Mascarella, S. W., Navarro, H. A., Rothman, R. B., Cantrell, B. E., Zimmerman, D. M., Thomas, J. B. |
| Zdroj: |
Journal of Medicinal Chemistry; January 2004, Vol. 47 Issue: 2 p281-284, 4p |
| Abstrakt: |
A structurally novel opioid δ receptor selective antagonist has been identified. This compound, (+)-5-(3-hydroxyphenyl)-4-methyl-2-(3-phenylpropyl)-2-azabicyclo[3.3.1]non-7-yl-(1-phenyl-1-cyclopentane)carboxamide [(+)-KF4, (+)-4], showed a Ke value of 0.15 nM in the [35S]GTPγS functional assay. (+)-KF4 is also a δ inverse agonist with an IC50 value of 1.8 nM. To our knowledge, this is the first potent and selective δ opioid receptor antagonist from the 5-phenylmorphan class of opioids. |
| Databáze: |
Supplemental Index |
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