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AssigneeFerring B.V.
InventorsJean Louis Junien, Pierre J.M. Riviere, Claudio D. Schteingart, Javier Sueiras Diaz, Jerzy A. Trojnar, Todd W. Vanderah
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Peptides which exhibit high selectivity for the kappa opioid receptor (KOR) and long duration of peripheral action without significant entry into the brain are created which are sequences of four D-isomer amino acid residues having a C-terminus which is a mono or di-substituted amide. Representative compounds, which have an affinity for the KOR at least 1,000 times their affinity for the mu opioid receptor and an ED.sub.50 of not greater than about 0.5 mg/kg, include H-D-Phe-D-Phe-D-Nle-D-Arg-NHEt, H-D-Phe-D-Phe-D-Nle-D-Arg-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NHPr, H-D-Phe-D-Phe-D-Nle-D-Arg-thiomorpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NEt.sub.2, H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe, H-D-Phe-D-Phe-D-Leu-D-Orn-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NHhEt, H-D-Phe-D-Phe-D-Nle-D-Arg-NH-cyclopropyl, H-D-Ala(2Thi)-D-4Cpa-D-Leu-D-Arg-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-piperidinyl, H-D-Phe-D-Phe-D-Leu-D-Orn-NHEt, H-D-Phe-D-Phe-D-Leu-D-Lys-morpholinyl, and H-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl.
A synthetic opioid peptide amide having an affinity for the kappa opioid receptor which is at least 1,000 times its affinity for the mu opioid receptor and which exhibits long duration of action when administered in vivo, which peptide has the formula:
A synthetic opioid peptide amide having an affinity for the kappa opioid receptor which is at least 1,000 times its affinity for the mu opioid receptor, and an WT-ED.sub.50 of about 0.5 mg/kg or less, and which exhibits long duration of action when administered in vivo, which peptide has the formula:
A synthetic opioid peptide amide having an affinity for the kappa opioid receptor which is at least 1,000 times its affinity for the mu opioid receptor and an ED.sub.50 of about 0.5 mg/kg or less, and which exhibits long duration of action when administered in vivo, which peptide has the formula:
Dependencies are inferred from the claim text.