Abstract: The C-terminal tetrapeptide of gastrin, Trp-Met-Asp-Phe-NH.sub.2, possesses gastrin pharmacological activity. Replacement of the methionyl moiety in the gastrin tetrapeptide, or its analogs, with a naphthylalanyl group produces compounds which interact with gastrin and/or cholecystokinin receptors, but have reduced gastrin and/or cholecystokinin agonist activity. Such partial agonists or antagonists of gastrin and/or cholecystokinin provide useful therapeutic agents.
Type:
Grant
Filed:
June 17, 1993
Date of Patent:
January 23, 1996
Assignee:
James Black Foundation Limited
Inventors:
Sarkis B. Kalindjian, Howard B. Broughton, Caroline M. R. Low, Iain M. McDonald, Robert A. D. Hull, Nigel P. Shankley, Ildiko M. Buck, Katherine I. M. Steel, Jonathan M. R. Davies
Abstract: Arylsulfonamide derivatives of .alpha.-amino dicarboxylic acids such as aspartic acid and glutamic acid posses anti-cholecystokinin activity. They are useful in the treatment of cholecystokinin-related disorders such as anorexia nervosa, pancreatic inflammation, biliary tract disease, Zollinger-Ellison syndrome and various psychiatric disorders, as well as in the potentiation of opiate analgesia, and in the treatment of certain cancers.
Type:
Grant
Filed:
January 12, 1993
Date of Patent:
March 21, 1995
Assignee:
James Black Foundation Limited
Inventors:
Howard B. Broughton, Sarkis B. Kalindjian, Caroline M. R. Low, Iain M. McDonald, Robert A. D. Hull, Nigel P. Shankley