In vitro labeling of serotonin-S2 receptors. Synthesis and binding characteristics of [3H]-7-aminoketanserin

…, CGM Janssen, J Van Dun, JBA Thijssen…

文献索引：Wouters, Walter; Janssen, Cornelus G. M.; Dun, Jacky Van; Thijssen, Jos B. A.; Laduron, Pierre M. Journal of Medicinal Chemistry, 1986 , vol. 29, # 9 p. 1663 - 1668

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被引用次数: 8

摘要

Conclusion In the series of 7cu-(l-hydroxy-l-methylphenalkyl) ori-pavines maximal analgesic activity has been reported to be associated with a 19-phenylpropyl chain as in PEO. The fact that analgesic potency is drastically reduced by shortening or lengthening the phenylalkyl chain implicates an additional well-defined binding site. We found that the conformation reported for the cyclic opioid peptide Hm-cyclo [-~-N~-Om-Gly-Phe-Leu-] provides the ...