发明授权
- 专利标题: CRF antagonists
- 专利标题(中): CRF拮抗剂
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申请号: US583092申请日: 1984-02-23
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公开(公告)号: US4605642A公开(公告)日: 1986-08-12
- 发明人: Catherine L. Rivier , Jean E. F. Rivier , Wylie W. Vale, Jr. , Marvin R. Brown
- 申请人: Catherine L. Rivier , Jean E. F. Rivier , Wylie W. Vale, Jr. , Marvin R. Brown
- 申请人地址: CA San Diego
- 专利权人: The Salk Institute for Biological Studies
- 当前专利权人: The Salk Institute for Biological Studies
- 当前专利权人地址: CA San Diego
- 主分类号: C07K1/06
- IPC分类号: C07K1/06 ; A61K38/00 ; A61K38/04 ; A61K38/22 ; A61P5/00 ; C07K1/02 ; C07K1/04 ; C07K14/00 ; C07K14/575 ; C07K7/10 ; A61K37/24
摘要:
Several polypeptide analogs of the known members of the corticotropin releasing factor (CRF) family have been synthesized and tested including human and rat CRF which have the formula: H-Ser-Glu-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Val-Leu-Glu-Met-Ala-Arg-Ala-Glu-Gln-Leu-Ala-Gln-Gln-Ala-His-Ser-Asn-Arg-Lys-Leu-Met-Glu-Ile-Ile-NH.sub.2. Peptides are herein disclosed that are potent competitive antagonists of CRF in mammals. One which has been found to be particularly potent is: H-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Met-Leu-Glu-Met-Ala-Lys-Ala-Glu-Gln-Glu-Ala-Glu-Gln-Ala-Ala-Leu-Asn-Arg-Leu-Leu-Leu-Glu-Glu-Ala-NH.sub.2. These antagonists or pharmaceutically or veterinarily acceptable salts thereof, dispersed in a pharmaceutically or veterinarily acceptable liquid or solid carrier, can be administered to mammals, including humans, to achieve a prevent elevation of ACTH, .beta.-endorphin, .beta.-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels and/or a lowering of brain-mediated responses to stress over an extended period of time. They may also be used to affect mood, memory and learning, as well as diagnostically.
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