Design and synthesis of highly potent and selective cyclic dynorphin A analogs

AM Kawasaki, RJ Knapp, TH Kramer…

Index: Kawasaki, Andrew M.; Knapp, Richard J.; Kramer, Thomas H.; Wire, William S.; Vasquez, Olga S.; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 7 p. 1874 - 1879

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Citation Number: 33

Abstract

We have designed and synthesized several cyclic disulfide-containing peptide analogues of dynorphin A (Dyn A) which are conformationally constrained in the putative" address" segment of the opioid ligand. Several of these Dyn A analogues exhibit unexpected selectivities for the K and p opioid receptors (s) of the central vs peripheral nervous systems. Thus, incorporation of conformational constraint in the putative" address" segment of Dyn ...