期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 48, 期 6, 页码 1713-1716出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm034234f
关键词
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资金
- NIDA NIH HHS [DA15091, DA01533] Funding Source: Medline
To characterize delta- and kappa-opioid receptor phenotypes, bivalent ligands (KDAN series) containing delta-antagonist (naltrindole) and kappa(1)-agonist (ICI-199,441) pharmacophores were synthesized and evaluated by the intrathecal route using the mouse tail-flick assay and binding studies. The data have suggested that KDAN-18 (2) bridges phenotypic delta(2)- and kappa(1)-receptors. A conceptual model is presented to explain the organizational differences between the opioid receptors that give rise to the phenotypes (delta(1), delta(2), kappa(1), kappa(2)).
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