Analogs of substance P and eledoisin

Details Analogs of substance P and eledoisin Analogs of substance P and eledoisin

1986-08-20

1987-07-14

Phillips, Delbert R.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

514 18, 530332, 530331, 530330, A61K 3702, C07K 702, C07K 508, C07K 510

Patent

active

046802835

ABSTRACT:
Analogs of substance P and eledoisin which are conformationally constrained by the presence of a lactam in the peptide chain demonstrate greater selectivity and increased protease stability and are useful as analgesic, anti-inflammatory, antihypertensive, central nervous system agents, and stimulants of lachrymal secretion. The compounds are prepared by standard peptide synthetic procedures.

REFERENCES:
patent: 4472305 (1984-09-01), Hansen et al.
DeCastiglione, Exploitation and Exploration of Ceruletide and Eledoisin, Biopolymers, 22, 507-515, (1983).
Sandberg & Iversen, Substance P, J. Med. Chem., 25, 1009, (1982).
Laufer et al., Persistent Action of N-methylated Analogs of Substance P on Rat Parotid Slices, FEBS. Letters, 123, 291, (1981).
Friedinger et al., Bioactive Conformation of Luteinizing Hormone-Releasing Hormone, Science, 210, 656-658, (1980).
The Peptides, vol. II, pp. 137-153, Synthesis, Occurence and Action of Biologically Active Polypeptides, Ed. E. Schroder & K. Lubke, (Academic Press, N.Y., 1966).
Freidinger et al., Protected Lactam-Bridged Dipeptides for Use as Conformational Constraints in Peptides, J. Org. Chem., 47, 104, (1982).
Substance P Metabolism & Biological Action, Piercey et al., ed. Jordan & Oehme, (London), 1985, (pp. 165-176).

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