カッパ受容体オピオイドペプチド

Title:

カッパ受容体オピオイドペプチド

Document Type and Number:

Japanese Patent JP4275852

Kind Code:

B2

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, includeH-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-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,andH-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl.

Inventors:

Junior jean louis
Riviere Pierre, Jay. M.
Steinguard Claudio Dee.
Diaz Javier Sueiras
Troyanal Jersey A.
Benderer Todd W.

Application Number:

JP2000525447A

Publication Date:

June 10, 2009

Filing Date:

December 22, 1998

Export Citation:

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Assignee:

Color Therapeutics, Inc.

International Classes:

A61K38/00; A61K38/07; C07K5/107; A61P1/04; A61P13/00; A61P13/10; A61P25/04; C07K5/10; C07K5/117

Domestic Patent References:

JP11220471A
JP3041092A
JP11512086A
JP9509168A
JP8507748A

Other References:

J. Biol. Chem., vol. 273, pages 18848-18856 (1998)
J. Pharmacol. Exp. Ther., vol. 310, pages 326-333 (2004)
Eur., J. Pharmacol., vol. 583, pages 62-72 (2008)

Attorney, Agent or Firm:

Yoshikazu Tani
Kazuo Abe

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