Detail of "171543-83-2"

Reference

Preparation and formulation of Urocortin peptides as pharmaceuticals

Preparation and formulation of Urocortin peptides as pharmaceuticals. Vale, Wylie W., Jr.; Vaughan, Joan; Donaldson, Cynthia J.; Lewis, Kathy A.; Sawchenko, Paul; Rivier, Jean E. F. 171543-83-2 and 9002-60-2 are also occured in this study.; Perrin, Marilyn H. (Salk Institute for Biological Studies; Vale, Wylie W., Jr.; Vaughan, Joan; Donaldson, Cynthia J.; Lewis, Kathy A.; Sawchenko, Paul; Rivier, Jean E. F.; Perrin, Marilyn H., USA). PCT Int. Appl. WO 9700063 A2 3 Jan 1997, 90 pp. DESIGNATED STATES: W: AL, AM, AT, AU, AZ, BB, BG, BR, BY, CA, CH, CN, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, NL, PT, SE. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: A61K. APPLICATION: WO 1996-US10240 12 Jun 1996. PRIORITY: US 1995-490314 13 Jun 1995; US 1995-2223 11 Aug 1995. DOCUMENT TYPE: Patent CA Section: 2 (Mammalian Hormones) Urocortin (Ucn) is a native mammalian peptide generally related to Urotensin I and ACTH Releasing Factor (CRF). Human Ucn has the formula: Asp-Asn-Pro-Ser-Leu-Ser-Ile-Asp-Leu-Thr-Phe-His-Leu-Arg-Thr-Leu-G lu-Leu-Ala-Arg-Thr-Gln-Ser-Gln-Arg-Glu-Arg-Ala-Glu-Gln-Asn-Arg-Ile-P he-Asp-Ser-Val-NH2. Rat-derived Ucn is identical but for 2 substitutions; asp2 for Asn2 and Pro4 for Ser4. Ucn or analogs thereof or pharmaceutically acceptable salts can be administered to humans and other mammals to achieve substantial elevation of ACTH, b-endorphin, b-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone. They can also be used to lower blood pressure over an extended period of time, as stimulants to elevate mood and to improve memory and learning performance, as well as diagnostically. Shortened fragments may be administered to release endogenous CRF and/or Ucn in the brain and peripherally. Ucn antagonists can be used to block the action of Ucn and/or CRF, as can antibodies to Ucn. Labeled Ucn agonists and antagonists can be used in drug screening assays along with CRF receptors; they may also be used diagnostically along with Ucn antibodies. .

Cardiovascular effects of long-term central and peripheral administration of urocortin, corticotropin-releasing factor, and adrenocorticotropin in sheep

Cardiovascular effects of long-term central and peripheral administration of urocortin, corticotropin-releasing factor, and adrenocorticotropin in sheep. Weisinger, R. S.; Blair-West, J. R.; Burns, P.; Denton, D. A.; Purcell, B.; Vale, W.; Rivier, J.; Weisinger, H. S.; May, C. N. (Howard Florey Institute of Experimental Physiology and Medicine, University of Melbourne, Parkville 3010, Australia). Endocrinology, 145(12), 5598-5604 (English) 2004 Endocrine Society. CODEN: ENDOAO. ISSN: 0013-7227. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) The neuroendocrine hormones ACTH and corticotropin-releasing factor (CRF), which are involved in the stress response, have acute effects on arterial pressure. New evidence indicates that urocortin (UCN), the putative agonist for the CRF type 2 receptor, has selective cardiovascular actions. The responses to long-term infusions of these hormones, both peripherally and centrally, in conscious animals have not been studied. Knowledge of the long-term effects is important because they may differ considerably from their acute actions, and stress is frequently a chronic stimulus. The present expts. investigated the cardiovascular effects of CRF, UCN, and ACTH in conscious sheep. 171543-83-2 and 86784-80-7 are cas registry numbers of chemicals which are used as reagents here. Infusions were made either into the lateral cerebral ventricles (icv) or i.v. over 4 d at 5 mg/h. UCN infused icv or iv caused a prolonged increase in heart rate (HR) and a small increase in mean arterial pressure (MAP). CRF infused icv or i.v. progressively increased MAP but had no effect on HR. Central administration of ACTH had no effect, whereas systemic infusion increased MAP and HR. In conclusion, long-term administration of these three peptides assocd. with the stress response had prolonged, selective cardiovascular actions. The striking finding was the large and sustained increase in HR with icv and i.v. infusions of UCN. These responses are probably mediated by CRF type 2 receptors because they were not reproduced by infusions of CRF. .