GRF Analogs III

Details GRF Analogs III GRF Analogs III

1983-10-25

1985-05-21

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

2601125R, C07C10352, A61K 3702

Patent

active

045185867

ABSTRACT:
Human parcreatic GRF(hpGRF), rat hypothalamic GRF(rGRF) and porcine hypothalamic GRF(pGRF) have been earlier characterized and synthesized. The invention provides synthetic peptides which are extremely potent in stimulating the release of pituitary GH in animals, including humans, which have resistance to enzymatic degradation in the body, and which have the sequence: R.sub.1 -R.sub.2 -R.sub.3 -Ala-Ile-Phe-Thr-R.sub.8 -Ser-R.sub.10 -Arg-R.sub.12 -R.sub.13 -Leu-R.sub.15 -Gln-R.sub.17 -R.sub.18 -Ala-Arg-Lys-Leu-R.sub.23 -R.sub.24 -R.sub.25 -Ile-R.sub.27 -R.sub.28 -Arg-Gln-Gln-Gly-Glu-R.sub.34 -Asn-Gln-Glu-R.sub.38 -R.sub.39 -R.sub.40 -Arg-R.sub.42 -R.sub.43 -R.sub.44 wherein R.sub.1 is Tyr, D-Tyr, Met, Phe, D-Phe, pCl-Phe, Leu, His or D-His having either a C.sup..alpha. Me or N.sup..alpha. Me substitution or being unsubstituted; R.sub.2 is Ala or D-Ala; R.sub.3 is Asp or D-Asp; R.sub.8 is Ser, Asn, D-Ser or D-Asn; R.sub.10 is Tyr or D-Tyr; R.sub.12 is Arg or Lys; R.sub.13 is Ile or Val; R.sub.15 is Gly or D-Ala; R.sub.17 is Leu or D-Leu; R.sub.18 is Tyr or Ser; R.sub.23 is Leu or D-Leu; R.sub. 24 is His or Gln; R.sub.25 is Glu, Asp, D-Glu or D-Asp; R.sub.27 is Met, D-Met, Ala, Nle, Ile, Leu, Nva or Val; R.sub.28 is Asn or Ser; R.sub.34 is Arg or Ser; R.sub.38 is Gln or Arg; R.sub.39 is Arg or Gly; R.sub.40 is Ser or Ala; R.sub.42 is Phe, Ala or Val; R.sub.43 is Asn or Arg; R.sub.44 is a natural amino acid; provided however that either R.sub.17 or R.sub.23 is D-Leu or R.sub.25 is either D-Glu or D-Asp and that any or all of the residues between R.sub.29 and R.sub.44, inclusive, may be deleted; or a nontoxic salt thereof. The carboxyl moiety of the amino acid residue at the C-terminus can be the radical --COOR,--CRO,--CONHNHR,--CON(R)(R') or --CH.sub.2 OR, with R and R' being lower alkyl, fluoro lower alkyl or hydrogen. These peptides as well as nontoxic salts thereof may be administered to animals, including humans and cold-blooded animals, to stimulate the release of GH and may be used diagnostically.

REFERENCES:
Science, Guillemin et al., "Growth Hormone-Releasing Factor from a Human Pancreatic Tumor that Caused Acromegaly", 11/5/82, vol. 218, pp. 585-587.
Nature, Spiess et al., "Characterization of Rat Hypothalamic Growth Hormone-Releasing Factor", vol. 303, Jun. 9, 1983, pp. 532-535.
8th American Peptide Symposium, Tucson, Arizona, May 22-27, 1983, p. 237, Abstract 10-B.
Biochemical and Biophysical Research Communications, Bohlen et al., "Isolation and Characterization of the Porcine Hypothalamic Growth Hormone Releasing Factor, vol. 116, No. 2, 1983, Oct. 31, 1983.
J. Spiess et al., Biochemistry, 21, 6037-6040, (1982).
F. S. Esch et al., Biochemical and Biophysical Research Communications, 109, No. 1, 152-158, (1982).
F. S. Esch et al., The Journal of Biological Chemistry, 258, No. 3, 1806-1810, (1983), Feb. 10 issue.

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