-transparent.png){kind=logo}
The tricyclic compound cyproheptadine (Periactinol, Nuran) inhibited glucose-induced insulin release from the perfused rat pancreas. Tolbutamide-stimulated insulin release was significantly reduced in the presence and completely suppressed in the absence of a substimulatory glucose concentration (5 mM). Arginine produced a slow rise of insulin release, which was completely abolished by cyproheptadine. Furthermore the biphasic glucagon release due to the stimulus was inhibited. Oxidation of 14C-glucose in isolated islets was unaltered in the presence of cyproheptadine, and pyruvate added to the perfusion medium failed to reverse the inhibitory effect on glucose induced insulin release, indicating that impaired glucose metabolism is not responsible for the inhibition. In addition, the inhibition remained unchanged when phentolamine was present, suggesting that the effect is not mediated by inhibitory adrenergic alpha receptors. Theophylline, in contrast, partly overcame the inhibition. When the calcium concentration of the medium was enhanced, the inhibitory effect of cyproheptadine was still visible, although the relative inhibition had become smaller. The results suggest that cyproheptadine blocks insulin release by affecting a fundamental step of the stimulus-secretion coupling common to peptide hormones. A participation of a calcium-antagonizing effect in the inhibition is discussed.
H G Joost, and
J Beckmann, and
S Holze, and
S Lenzen, and
W Poser, and
A Hasselblatt
January 1974,
Naunyn-Schmiedeberg's archives of pharmacology,
H G Joost, and
J Beckmann, and
S Holze, and
S Lenzen, and
W Poser, and
A Hasselblatt
December 1983,
European journal of pharmacology,
H G Joost, and
J Beckmann, and
S Holze, and
S Lenzen, and
W Poser, and
A Hasselblatt
January 1982,
Peptides,
H G Joost, and
J Beckmann, and
S Holze, and
S Lenzen, and
W Poser, and
A Hasselblatt
September 1987,
Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme,
H G Joost, and
J Beckmann, and
S Holze, and
S Lenzen, and
W Poser, and
A Hasselblatt
July 1975,
Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme,
H G Joost, and
J Beckmann, and
S Holze, and
S Lenzen, and
W Poser, and
A Hasselblatt
March 1993,
Hormone and metabolic research = Hormon- und Stoffwechselforschung = Hormones et metabolisme,
H G Joost, and
J Beckmann, and
S Holze, and
S Lenzen, and
W Poser, and
A Hasselblatt
August 1990,
Diabetes,
H G Joost, and
J Beckmann, and
S Holze, and
S Lenzen, and
W Poser, and
A Hasselblatt
June 1983,
Diabetes,
H G Joost, and
J Beckmann, and
S Holze, and
S Lenzen, and
W Poser, and
A Hasselblatt
September 2002,
Metabolism: clinical and experimental,
H G Joost, and
J Beckmann, and
S Holze, and
S Lenzen, and
W Poser, and
A Hasselblatt
August 1989,
Endocrinologia japonica,
