Analogs of extended N-terminal somatostatin

Drug – bio-affecting and body treating compositions – Immunoglobulin – antiserum – antibody – or antibody fragment,... – Reduced antigenicity – reduced ability to bind complement – or...

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2601125S, A61K 3700, C07C10352

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active

043930506

ABSTRACT:
Somatostatin-28 has the formula: ##STR1## Analogs have been synthesized that are more potent than somatostatin-28, and these analogs or pharmaceutically acceptable salts thereof, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals in the same manner as somatostatin. In the analogs, Leu may be substituted in the 8-position in combination with D-Trp in the 22-position and/or Tyr in the 25-position. D-Cys may also be substituted in the 28-position, and D-Ser may be substituted in the 27-position. Certain residues may also be deleted. D-Trp.sup.22 somatostation-28 has surprisingly been found to be insulin-selective when administered in vivo and is useful for the treatment of insulinoma.

REFERENCES:
patent: 4316891 (1982-02-01), Guillemin et al.
FEBS Letters, Jan. 1980, vol. 109, No. 1, Biochem, and Biophys. Res. Comm., vol. No. 95, No. 3, pp. 945-951, 8/14/80 Ling et al. "Solid Phase Synthesis of Somatostatin-28.
Biochem. and Biophys. Res. Comm., vol. 96, No. 2, pp. 725-734, 9/30/80, Bohlen et al. "Isolation and Amino Acid Composition of Two Somatostatin-Like Peptides from Ovine Hypothalamus": Somatostatin-28 and Somatostatin-25.

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