CRF-ANALOGA

• Main Authors: RIVIER, JEAN EDOUARD FREDERIC, BROWN, MARVIN ROSS, RIVIER, CATHERINE LAURE, VALE, WYLIE WALKER
• Format: Patent
• Language: English; German
• Published: 15.05.1993
• Edition: 5
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Agonists of rCRF and oCRF are disclosed that can be administered to achieve a substantial elevation of ACTH. ß-endorphin, ß-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels and/or a lowering of blood pressure over an extended period of time. One agonist which has been found to be particularly potent is: H-Ser-Gln-Glu-Pro-Pro-Ile-Ser-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-NH2. In the agonists, one or more of the first five N-terminal residues may be deleted or may be substituted by a peptide up to 10 amino acids long and cr by an acylating agent containing up to 7 carbon atoms. A number of other substitutions may also be made throughout the chain. Similar peptides which function as CRF antagonists are ceated by deleting the first 7, 8 or 9 N-terminal residues. These analogs or pharmaceuncally or veterinarily acceptable salts thereof, dispersed in a pharmaceutically or veterinarily acceptable liquid or solid carrier can be administered to mammals, including humans The agonists may also be used as stimulants to elevate mood and improve memory and teaming, as well as diagnostically. The antagonists can be used to lower stress.