K receptor opioid peptides

A technology of opioid peptides and opioid substances, applied in the field of synthetic opioid peptides, can solve problems such as polyuria
CN1154655CInactive Publication Date: 2004-06-23CARA THERAPEUTICS
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CARA THERAPEUTICS
Publication Date
2004-06-23
Estimated Expiration
Not applicable · inactive patent

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Abstract

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 ED50 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-NEt2, H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe, H-D-Phe-D-Phe-D-Leu-D-Orn-morpholinyl, H-D-4Fpa-D-Phe-D-Nle-D-Arg-NH-4-picolyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NH-cyclopropyl, H-D-Ala-(2Thi)-D-3, 4Cpa-D-Leu-D-Arg-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Gmf-morpholinyl, H-D-Phe-D-Phe-D-Leu-D-Orn-NH(Aeb), H-D-Phe-D-Phe-D-Leu-D-Lys-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl, and H-D-Phe-D-Phe-D-Nle-D-Arg-NH(Hoh).
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Description

[0001] The present invention mainly relates to synthetic opioid peptides, specifically to opioid peptides as highly selective κ receptor activators, and more specifically to activators that (a) do not penetrate into the brain, and (b) ) Has long-term anti-nociceptive activity in vivo. Background of the invention

[0002] Kappa opioid receptors (KOR) exist in the brain, spinal cord, central and peripheral nerve endings, (somatic and visceral) primary sensory afferent nerve cell bodies, and immune cells. Molecules that activate KOR are generally called kappa activators.

[0003] It is known that activating KOR in the brain can produce analgesic effects. Based on this discovery, people tried to develop brain-permeable non-peptide κ activators as new analgesics to avoid the side effects (constipation, respiratory depression) of morphine analogs acting on the mu opioid receptor (MOR) , Dependence and addiction). It has been confirmed in animals and humans tha...

Claims

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