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US 2017/0362276 A1Published application
Mu opioid receptor agonist analogs of the endomorphins
AssigneesThe Administrators of the Tulane Educational Fund, United States Department of Veterans Affairs
InventorsJames E. ZADINA, Laszlo HACKLER
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Abstract
The invention relates to cyclic peptide agonists that bind to the mu (morphine) opioid receptor and their use in the treatment of acute and/or chronic pain. Embodiments of the invention are directed to cyclic analogs of endomorphin. These peptide analogs exhibit decreased tolerance relative to morphine, increased solubility compared to similar tetrapeptide analogs, while maintaining favorable or improved therapeutic ratios of analgesia to side effects.
Claims15
A cyclic peptide of Formula I:
- H-Tyr-cyclo[X1-X2-X3-X4]-X5 (I),
- wherein
- X1 is a basic D-amino acid;
- X2 is Trp;
- X3 is an aromatic amino acid;
- X4 is an acidic amino acid;
- X5 is selected from the group consisting of Ala-NHR, Arg-NHR, Asn-NHR, Asp-NHR, Cys-NHR, Glu-NHR, Gln-NHR, Gly-NHR, His-NHR, Ile-NHR, Leu-NHR, Met-NHR, Orn-NHR, Phe-NHR, Pro-NHR, Ser-NHR, Thr-NHR, Trp-NHR, Tyr-NHR, and Val-NHR, wherein R is H or an alkyl group;
- and
- there is an amide bond between an amino group and a carboxylic acid group on side chains of amino acids X1 and X4.
6 more elements
Dependencies are inferred from the claim text.