科研之友
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摘要
The cyclic dimers of enkephalin were isolated as minor components during the solution synthesis of the corresponding cyclic monomers. The ratio of cyclic dimer to monomer was approximately 1:4 from the percent of yields. In the receptor binding assay of two cyclic dimmers, (Tyr(2)-C[D-Glu-Phe-gPhe](2) 6, Tyr(2)-C[D-Asp-Phe-gPhe-rLeu](2) 8), both analogs exhibited the high preference for 5 receptor compared to monocyclic counterparts. In the nociceptive activity, both showed about 5 times less potent than the cyclic monomers. The repeated synthesis of 14-membered cyclic analog, Tyr-C[D-Glu-Phe-gPhe-D-rLeu] 14, which was known as having three distinct cis-trans isomers, gave rise to apparently different conformational analog arousing only trans isomer. In the receptor binding assay, it showed tremendously high selectivity toward mu receptor (delta/mu = 160).
- 出版日期2012-1-20
