.mu.opioid receptor ligands: agonists and antagonists

Details .mu.opioid receptor ligands: agonists and antagonists .mu.opioid receptor ligands: agonists and antagonists

1995-06-07

1997-06-24

Cain, Edward J.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

6 to 7 amino acid residues in defined sequence

A61K 3808, A61K 3804

Patent

active

056418612

ABSTRACT:
The present invention provides novel opioid peptides. Disclosed are opioid peptides having the general structures Ac-Phe-Arg-Trp-Trp-Tyr-Xaa--NH.sub.2 (SEQ ID NO. 1); Ac-Arg-Trp-Ile-Gly-Trp-Xaa--NH.sub.2 (SEQ ID NO. 2); Trp-Trp-Pro-Lys-His-Xaa--NH.sub.2 (SEQ ID NO. 3); and shorter versions of the latter, namely, Trp-Trp-Pro-Xaa--NH.sub.2 (SEQ ID NO. 4); Tyr-Pro-Phe-Gly-Phe-Xaa--NH.sub.2 (SEQ ID NO. 5); (D)Ile-(D)Met-(D)Ser-(D)Trp-(D)Trp-Gly.sub.n -Xaa--NH.sub.2 (SEQ ID NO. 6); and (D)Ile-(D)Met-(D)Thr-(D)Trp-Gly-Xaa--NH.sub.2 (SEQ ID NO. 7). Within each genus, Xaa is substituted by a specific amino acid. The invention also relates to an opioid peptide having the general structure Tyr-A1-B2-C3--NH.sub.2 (SEQ ID NO. 214), wherein A is D-Nve or D-Nle, B is Gly, Phe, or Trp, and C is Trp or Nap. Also included within the invention are opioid peptides of the general structure Pm and red {Me.sub.x H.sub.y N-Tyr-(NMe).sub.z -Tyr-Xaa.sub.z --NH.sub.2 } (SEQ ID NO. 221), wherein Xaa is substituted by a specific amino acid.

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