Polypeptide analgesics

C - Chemistry – Metallurgy – 07 – K

Patent

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530/7.12

C07K 16/26 (2006.01) C07K 14/665 (2006.01) G01N 33/68 (2006.01) G01N 33/94 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1177825

NOVEL POLYPEPTIDE ANALGESICS ABSTRACT OF THE DISCLOSURE Novel opioid compounds are provided having a phenolic hydroxyl and a pentet of alternating basic hydrophilic and hydrophobic groups derived from basic amino acids and hydrophobic amino acids. Desirably, the pentet, usually sextet, is separated from the phenolic ring by at least about 3 atoms in a chain, preferably at least about 15 atoms in a chain and not more than about 30 atoms in a chain (for rings one will take the average of the shortest and longest distances). Particularly, a polypeptide is provided having tyrosyl at the amine end, desirably as the first amino acid of leu- or met- enkephalin and a sextet of alternating basic hydrophilic and hydrophobic amino acids spaced from the enkephalin by at least about one amino acid. Desirably, the poly- peptide is at least 1,200 molecular weight and under about 2,500 molecular weight.

363326

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