Novel kappa receptor selective opioid peptides

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 7/06 (2006.01) A61K 38/08 (2006.01) A61K 38/33 (2006.01) C07K 5/103 (2006.01) C07K 5/107 (2006.01) C07K 14/665 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2223176

The present invention provides novel opioid peptides which are selective for the kappa opiate receptor. In one embodiment, the kappa-selective opioid peptides have the general structure Ac-A1-B2-C3-Arg-Tyr- Arg-Tyr-Arg-Arg-Arg-NH2, (SEQ ID NO. 28), wherein A1 is Tyr or Arg, B2 is Arg or Phe, and C3 is Thr, Phe, or Met. In yet other embodiments, the kappa-selective opioid peptides have the general structure (D)Phe-D4-E5-F6 (SEQ ID NO. 29) or (D)Nle-D4-E5-F6 (SEQ ID NO. 30), where in both of these formulae D4 is (D)NapAla or (D)Phe, E5 is (D)Nle, Trp, or (D)Ile, and F6 is (D)Arg or (D)ChAla.

Nouveaux peptides opioïdes sélectifs vis-à-vis du récepteur opiacé kappa. Dans un mode de réalisation, ces peptides présentent la structure générale Ac-A1-B2-C3-Arg-Tyr-Arg-Tyr-Arg-Arg-Arg-NH2 (SEQ ID No. 28), dans laquelle A1 représente Tyr ou Arg, B2 représente Arg ou Phe, and C3 représente Thr, Phe ou Met. Dans d'autres modes de réalisation, lesdits peptides présentent la structure générale (D)Phe-D4-E5-F6 (SEQ ID No. 29) ou (D)Nle-D4-E5-F6 (SEQ ID No. 30), dans lesquelles D4 représente (D)NapAla ou (D)Phe, E5 représente (D)Nle, Trp ou (D)Ile, et F6 représente (D)Arg ou (D)ChAla.

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