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

Full Text: HTML

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 ...

Related Articles:

Design, synthesis, and biological activities of cyclic lactam peptide analogues of Dynorphin A (1-11)-NH2 1

[Lung; Collins; Stropova; Davis; Yamamura; Porreca; Hruby Journal of Medicinal Chemistry, 1996 , vol. 39, # 5 p. 1136 - 1141]

[2', 6'-Dimethyltyrosine] Dynorphin A (1-11)-NH2 Analogues Lacking an N-Terminal Amino Group: Potent and Selective κ Opioid Antagonists

[Lu; Nguyen; Weltrowska; Berezowska; Lemieux; Chung; Schiller Journal of Medicinal Chemistry, 2001 , vol. 44, # 19 p. 3048 - 3053]

More Articles...