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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 33, Number 1
BKCSDE 33(1)
January 20, 2012 

Activity Profiles of Linear, Cyclic Monomer and Cyclic Dimer of Enkephalin
Dong Hee Kim, Nam Joo Hong *
Cyclic-enkephalin, Monomer, Dimer, Bioactivity
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, (Tyr2-C[D-Glu-Phe-gPhe]2 6, Tyr2-C[D-Asp- Phe-gPhe-rLeu]2 8), both analogs exhibited the high preference for δ 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 μ receptor (δ/μ = 160).
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