Analogs of extended N-terminal somatostatin
AssigneeThe Salk Institute for Biological Studies
InventorsWylie W. Vale, Jr., Jean E. F. Rivier, Marvin R. Brown
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AssigneeThe Salk Institute for Biological Studies
InventorsWylie W. Vale, Jr., Jean E. F. Rivier, Marvin R. Brown
Estimating the term…
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.
A pharmaceutical composition for decreasing gastric acid secretion comprising an effective amount of an analog of SS-28 having the formula:
A method of inhibiting the release of growth hormone, insulin, adrenal epenephrine and or glucagon in a mammal or modifying the temperature regulation or the gastrointestinal function of a mammal, which method comprises administering to said mammal an effective amount of a material selected from the class consisting of analogs of SS-28 having the formula:
##STR8## wherein R.sub.18 is Lys or des R.sub.18, R.sub.19 is Asn or des R.sub.19, R.sub.25 is Phe or Tyr, R.sub.26 is Thr or des R.sub.26, R.sub.27 is Ser or D-Ser and R.sub.28 is D--Cys or Cys, or the linear version thereof where the disulfide bridge is replaced by hydrogen.
##STR9## wherein R.sub.8 is Met or Leu, R.sub.18 is Lys or des R.sub.18, R.sub.19 is Asn or des R.sub.19, R.sub.25 is Phe or Tyr, R.sub.26 is Thr or des R.sub.26, R.sub.27 is Ser or D-Ser and R.sub.28 is D-Cys or Cys, provided however that when R.sub.27 is Ser, R.sub.28 is D-Cys, or the linear version thereof where the disulfide bridge is replaced by hydrogen.
Dependencies are inferred from the claim text.