Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 5, Issue 9, Pages 1032-1036Publisher
AMER CHEMICAL SOC
DOI: 10.1021/Ml500241n
Keywords
Analgesics; biphalin; dimeric opioid peptides; cyclic analogues
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Two novel opioid analogues have been designed by substituting the native d-Ala residues in position 2,2' of biphalin with two residues of d-penicillamine or l-penicillamine and by forming a disulfide bond between the thiol groups. The so-obtained compound 9 containing d-penicillamines showed excellent mu/delta mixed receptor affinities (K-i(delta) = 5.2 nM; K-i mu = 1.9 nM), together with an efficacious capacity to trigger the second messenger and a very good in vivo antinociceptive activity, whereas product 10 was scarcely active. An explanation of the two different pharmacological behaviors of products 9 and 10 was found by studying their conformational properties.
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