During the 1960s at Rotta Research Laboratorium, Rovati [1] developed a gastrin receptor antagonist named proglumide, i.e., DL-4-benzamido-N, N-dipropyl-glutaramic acid. Proglumide has been used for several years for the treatment of peptic ulcer.


Pancreatic Acinus Experimental Pancreatitis Gastrin Receptor Cholecystokinin Antagonist Cholecystokinin Receptor Antagonist 
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  1. 1.
    Rovati AL (1968) The relationship between chemical structure of a new dicarboxylic amino-acid derivative and antigastrin activity in the rat. Br J Pharmacol 34:677–682Google Scholar
  2. 2.
    Hahne WF, Jensen RT, Lemp GF, Gardner JD (1981) Proglumide and benzotript: members of a different class of cholecystokinin receptor antagonists. Proc Natl Acad Sci USA 78:6304–6308PubMedCrossRefGoogle Scholar
  3. 3.
    Makovec F, Chistè R, Bani M, Revel L, Setnikar I, Rovati AL (1986) New glutamic and aspartic derivatives with potent CCK-antagonistic activity. Eur J Med Chem 21:9–20Google Scholar
  4. 4.
    Makovec F, Chistè R, Bani M, Pacini MA, Setnikar I, Rovati LA (1985) New glutaramic acid derivatives with potent, competitive and specific, cholecystokinin-antagonistic activity. Arzneimittelforschung 35:1048–1051PubMedGoogle Scholar
  5. 5.
    Setnikar I, Bani M, Cereda R, Chistè R, Makovec F, Pacini MA, Revel L, Rovati LC, Rovati LA (1987) Pharmacological characterization of a new potent and specific nonpolypeptidic cholecystokinin antagonist. Arzneimittelforschung 37:703–707PubMedGoogle Scholar
  6. 6.
    Makovec F, Bani M, Chistè R, Revel L, Rovati LC, Rovati LA (1986) Differentiation of central and peripheral cholecystokinin receptors by new glutaramic acid derivatives with cholecystokinin-antagonistic activity. Arzneimittelforschung 36:98–102PubMedGoogle Scholar
  7. 7.
    Jensen RT, Zhon ZC, Murphy RB, Jones SW, Setnikar I, Rovati LA, Gardner JD (1986) Structural features of various proglumide-related cholecystokinin receptor antagonists. Am J Physiol 251:G839–G846PubMedGoogle Scholar
  8. 8.
    Makovec F, Bani M, Cereda R, Chisté R, Pacini MA, Revel L, Rovati LC (1987) Antispasmodic activity on the gallbladder of the mouse of CR 1409 (lorglumide) a potent antagonist of peripheral CCK. Pharmacol Res Commun 19:41–51PubMedCrossRefGoogle Scholar
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    Makovec F, Bani M, Cereda R, Chisté R, Pacini MA, Revel L, Rovati LA, Rovati LC, Setnikar I (1987) Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung 37:1265–1268PubMedGoogle Scholar
  10. 10.
    Setnikar I, Bani M, Cereda R, Chisté R, Makovec F, Pacini MA, Revel L (1987) Anticholecystokinin activities of loxiglumide. Arzneimittelforschung 37: 1168–1171PubMedGoogle Scholar
  11. 11.
    Rovati LC, Bani M, Makovec F, Revel L, Setnikar I (1987) Lorglumide and loxiglumide: two potent and specific antagonists of peripheral CCK. Excerpta Med Int Congr Ser 766:45–48Google Scholar
  12. 12.
    Makovec F, Bani M, Chisté R, Revel L, Rovati LC, Setnikar I (1986) Different peripheral and central antagonistic activity of new glutaramic acid derivatives on satiety induced by cholecystokinin in rats. Regul Pept 16:281–290PubMedCrossRefGoogle Scholar
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    Makovec F, Bani M, Cereda R, Chisté R, Revel L, Rovati LC, Setnikar I, Rovati LA (1986) Protective effect of CR 1409 (cholecystokinin antagonist) on experimental pancreatitis in rats and mice. Peptides 7:1159–1164PubMedCrossRefGoogle Scholar
  14. 14.
    Setnikar I, Bani M, Cereda R, Chisté R, Pacini MA, Revel L (1987) Loxiglumide protects against experimental pancreatitis. Arzneimittelforschung 37:1172–1174PubMedGoogle Scholar
  15. 15.
    Setnikar I, Chisté R, Makovec F, Rovati LC, Warrington SJ (1988) Pharmacokinetics of loxiglumide after single intravenous or oral doses in man. Arzneimittelforschung 38:716–720PubMedGoogle Scholar
  16. 16.
    Setnikar I, Chisté R, Giacovelli G, Rovati LC (1989) Pharmacokinetics and tolerance of repeated oral doses of loxiglumide. Arzneimittelforschung 39: 1454–1459PubMedGoogle Scholar
  17. 17.
    Meyer BM, Werth BA, Beglinger C, Hildebrand P, Jansen JBMJ, Zach D, Rovati LC, Stalder GA (1989) Role of cholecystokinin in regulation of gastrointestinal motor functions. Lancet 2:12–15PubMedCrossRefGoogle Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 1991

Authors and Affiliations

  • L. C. Rovati
    • 1
  1. 1.Department of Clinical PharmacologyRotta Research LaboratoriumMonza (Milano)Italy

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