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. 1978 Sep;64(1):99–108. doi: 10.1111/j.1476-5381.1978.tb08646.x

A new bioassay for glucagon

G Gagnon, D Regoli, F Rioux
PMCID: PMC1668257  PMID: 698487

Abstract

1 The relaxant action of glucagon has been studied in strips of rabbit renal arteries partially contracted by a low concentration (1 ng/ml) of noradrenaline.

2 The preparation was relaxed in a dose-dependent manner by concentrations of glucagon varying between 25 ng/ml and 420 ng/ml.

3 The relaxant effect of glucagon (0.1 μg/ml ≃ ED60) on this preparation was not affected by propranolol (5.0 μg/ml), cimetidine (10 μg/ml), diphenhydramine (10 μg/ml), indomethacin (5.0 μg/ml), phentolamine (1.2 μg/ml), atropine (10 μg/ml) and 8-Leu-ATII (1.0 μg/ml) but was slightly potentiated by Des-Arg9 Leu-OMe8-Bk (25 μg/ml) and indomethacin (50 μg/ml).

4 The dose-response curve to glucagon remained parallel in the presence of papaverine (2.5 μg/ml) but was shifted to the left by a factor of 2.5 to 2.8. Theophylline (250 μg/ml) also potentiated the vascular relaxation induced by glucagon.

5 Insulin (10 μg/ml) did not influence the relaxant effect of glucagon.

6 The removal of the N-terminal amino acid (His) of glucagon reduced by 89% the biological activity of this fragment on the vascular preparation. The removal of the C-terminal amino acids Met-27, Asn-28 and Thr-29 of glucagon resulted in a fragment which was inactive either as an agonist or as an antagonist when tested at concentrations as high as 925 ng/ml.

7 It is concluded that the relaxation of partially contracted strips of rabbit renal arteries by glucagon constitutes a simple, sensitive, relatively specific and reliable bioassay which may be useful for the determination of glucagon in biological materials and for structure-activity relationship studies with this hormone.

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Selected References

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