| Endomorphin analogues with balanced affinity for bothμ- andδ-opioid receptors |
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| 作者姓名： | Lawrence H.Lazarus |
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| 作者单位： | a School of Pharmacy, Nanjing Medical University, Nanjing 210029, China;b Medicinal Chemistry Group, Laboratory of Toxicology and Pharmacology, National Institute of Environmental Health Sciences, Research Triangle Park, NC 27709, USA |
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| 基金项目： | was supported by grants 08KJB350002 and 08NMUZ028; in part by the Intramural Research Program of the NIH and NIEHS |
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| 摘 要： | Analogues of endomorphin and tripeptidcs modified at positions 4 and 3,respectively,with various phenylalanine analogues were synthesized and their affinities for opioid receptors were evaluated.Most of the peptides exhibited potentμ-receptor affinity and selectivity,among them,compound 7(Dmt-Pro-Tmp-Tmp-NH_2) exhibited potent affinity for bothμ-andδ-receptors (K_iμ= 0.47 nmol/L,K_iδ= 1.63 nmol/L).
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