Glucagon-like peptide-1(7-37) has a larger volume of distribution than glucagon-like peptide-1(7-36)amide in dogs and is degraded more quickly in vitro by dog plasma

European Journal of Drug Metabolism and Pharmacokinetics

Volumn 21, Issue 1, 1996, Pages 51-59

  Pridal, L ^a   Deacon, C F ^b   Kirk, O ^a   Christensen, J V ^a   Carr, R D ^a   Holst, J J ^b  

^a NOVO NORDISK A S   (Denmark)

^b UNIVERSITY OF COPENHAGEN   (Denmark)

Author keywords

GLP 1(7 36)amide; GLP 1(7 37); Glucagon like peptide 1; Metabolites; Pharmacokinetics

Indexed keywords

BACITRACIN; GLUCAGON LIKE PEPTIDE; GLUCAGON LIKE PEPTIDE 1 [7-36] AMIDE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DIAGNOSTIC ACCURACY; DOG; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DEGRADATION; DRUG DISTRIBUTION; DRUG RETENTION; ENZYME LINKED IMMUNOSORBENT ASSAY; FEMALE; INTERMETHOD COMPARISON; INTRAVENOUS DRUG ADMINISTRATION; MALE; NONHUMAN; PLASMA; PLASMA CLEARANCE; PLASMA HALF LIFE; RADIOIMMUNOASSAY; SUBCUTANEOUS DRUG ADMINISTRATION;

EID: 0030017161     PISSN: 03787966     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF03190278     Document Type: Article

References (16)

1. Ørskov C. (1992) : Glucagon-like peptide-1, a new hormone of the entero-insular axis. Diabetologica, 35, 701-711.
2. Ørskov C., Wettergren A , Rabenhøj L., Hoist J.J. (1993) : A comparison of the production, secretion and effects of glucagon-like peptide-1(7-36)amide and GLP-1(7-37). Digestion, 54, 382-383.
3. Mojsov S., Kopczynski M.G., Habener J.F. (1990) : Both amidated and nonamidated forms of glucagon-like peptide-1 are synthesized in the rat intestine and pancreas. J. Biol. Chem., 265, 8001-8008.
4. Buckley D.I, Lundquist P. (1992) : Analysis of the degradation of insulinotropin [GLP-1(7-37)] in human plasma and production of degradation resistant analogs. Regul. Pept., 40, 117A.
5. Deacon C.F., Johnsen A.H., Hoist J.J. (1995) : Degradation of glucagon-like peptide-1 by human plasma in vitro yields an N-terminally truncated peptide which is a major endogenous metabolite in vivo. J. Clin. Endocrinol. Metab., 80, 952-957.
6. Rachman J, Turner R.C. (1995) : Drugs on the horizon for treatment of type II diabetes. Diabetic Med., 12, 467-478.
7. Galloway J.A., Chance R.E. (1994) : Improving insulin therapy: achievements and challenges. Horm. Metab. Res., 26, 591-598.
8. Ørskov C., Wettergren A., Hoist J.J. (1993) : Biological effects and metabolic rates of glucagon-like peptide-1 (7-36)amide and glucagon-like peptide-1(7-37) in healthy subjects are indistinguishable. Diabetes, 42, 658-661.
9. Deacon C.F., Nauck M.A., Ton-Nielsen M, Pridal L., Wilims B., Hoist J.J. (1995) : Both subcutaneously and intravenously administered glucagon-like peptide-1 are rapidly degraded from the amino terminus in type II diabetic patients and healthy subjects. Diabetes, 44, 1126-1131.
10. Adelhorst K., Hedegaard B.B., Knudsen L.B., Kirk O. (1994) : Structure-activity studies of glucagon-like peptide-1. J. Biol. Chem., 269, 6275-6278.
11. Pridal L., Ingwersen S.H., Larsen F.S., Hoist J.J., Adelhorst K., Kirk O. (1995) : Comparison of sandwich enzyme-linked immunoadsorbent assay and radioimmunoassay for determination of exogenous glucagon-like peptide-1(7-36)amide in plasma. J. Pharm. Biomed. Anal., 13, 841-850.
12. Hoist J.J., Bersani M, Johnsen A.H., Kofod H., Hartmann B., Ørskov C. (1994) : Proglucagon processing in the porcine and human pancreas. J. Biol. Chem., 269, 18827-18833.
13. Heinzel G., Woloszczak R., Thomann P. (1993) : Pharmacokinetic and pharmacodynamic data analysis system for the PC. Topfit 2.0. Stuttgart, Gustav Fischer.
14. Rowland M., Tozer T.N. (1989) : Clinical Pharmacokinetics, Concepts and Applications, 2nd edn. Philadelphia, Lea & Febiger, p. 143.
15. Knudsen L.B., Pridal L. (1995) : Glucagon-like peptide-1 (9-36)amide is a major metabolite of glucagon-like peptide-1 (7-36)amide after in vivo administration to dogs, and it acts as an antagonist on the pancreatic receptor. Eur J. Pharmacol. (in press).
16. Uttenthal L.O, Ghiglione M., Van Delft J., Hermida O.G., Fontela T., Koch C. (1993) : A sensitive enzyme-linked immunosorbent assay for glucagon-like peptide-1. Digestion, 54, 395.