CRF analogs

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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Details

530324, 530302, 530306, 436817, C07K 700, A61K 3702, G01N 3354

Patent

active

045943290

ABSTRACT:
Analogs of rCRF and oCRF are disclosed that can be administered to achieve a substantial elevation of ACTH, .beta.-endorphin, .beta.-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 analog 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-NH.sub.2. In the analogs, 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/or by an acylating agent containing up to 7 carbon atoms. A number of other substitutions may also be made throughout the chain. These analogs 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. These analogs may also be used as stimulants to elevate mood and improve memory and learning, as well as diagnostically.

REFERENCES:
patent: 4415558 (1983-11-01), Vale, Jr. et al.
Yasuda et al., Biochemical Biophysical Research Communications, 81, No. 4, 1187-1194 (1978).
Chemical Abstracts, 101, 85 (1984) Abst. No. 33565v.
Chemical Abstracts, 101, 96 (1984) Abst. No. 144371y.
Rivier, et al., Characterization of Rat Hypothalamic Corticotropin-Releasing Factor, Proc. Natl. Acd. Sci., USA, vol. 80, pp. 4851-4855, Aug. 1983.
Spiess, et al., Sequence of Rat Hypothalamic Corticotropin-Releasing Factor with the o-Phthalaldehyde Strategy, Biochemistry vol. 22, pp. 4341-4346, 1983.

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