Receptor selective analogues of cholecystokinin-8
AssigneeArizona Technology Development Corporation
InventorsSunan Fang, Victor Hruby
Life of this patent
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Abstract
Analogues of cholecystokinin-8, which are receptor selective, vary from the normal hormone by alteration of at least one of the two, three or six position amino acids of the natural sequence.
Claims8
A receptor selective analogue of cholecystokinin-8, having the amino acid sequence ##STR2## wherein X is Tyr or Dopa
- Y is N-MeNle, Val, D-Val, Phe or D-Phe
- Z is Nle or N-MeNle, and
- M is H or --SO.sub.3.sup.-, and exhibiting a pancreatic receptor/brain receptor selectivity ratio, measured by .sup.125 I-cholecystokinin-8 binding inhibition, of less than 0.40 or in excess of 30.
A receptor selective analogue of cholecystokinin-8, having a biological activity of cholecystokinin-8 and exhibiting a pancreatic receptor/brain receptor selectivity ratio, measured by .sup.125 I-cholecystokinin-8 binding inhibition, of less than 0.40 or in excess of 30, having residues of the peptide ##STR3## wherein Z=N-MeNle.
A receptor selective analogue of cholecystokinin-8, having the amino acid sequence ##STR4## wherein X is Tyr or Dopa
- Y is Nle, N-MeNle, Val, D-Val, Phe or D-Phe
- Z is N-MeNle, and
- M is H or --SO.sub.3.sup.-, and exhibiting a pancreatic receptor/brain receptor selectivity ratio, measured by .sup.125 I-cholecystokinin-8 binding inhibition, of less than 0.40 or in excess of 30.
A receptor selective analogue of cholecystokinin-8, having the amino acid sequence ##STR5## wherein X is Dopa
- Y is Nle, N-MeNle, Val, D-Val, Phe or D-Phe
- Z is Nle or N-MeNle, and
- M is H or --SO.sub.3.sup.-, and exhibiting a pancreatic receptor/brain receptor selectivity ratio, measured by .sup.125 I-cholecystokinin-8 binding inhibition, of less than 0.40 or in excess of 30.
Dependencies are inferred from the claim text.