TY - JOUR
T1 - Repaglinide at a cellular level
AU - Krogsgaard Thomsen, M
AU - Bokvist, K
AU - Høy, M
AU - Buschard, K
AU - Holst, J J
AU - Lindström, P
AU - Gromada, J
PY - 2002/12
Y1 - 2002/12
N2 - To investigate the hormonal and cellular selectivity of the prandial glucose regulators, we have undertaken a series of experiments, in which we characterised the effects of repaglinide and nateglinide on ATP-sensitive potassium ion (KATP) channel activity, membrane potential and exocytosis in rat pancreatic alpha-cells and somatotrophs. We found a pharmacological dissociation between the actions on KATP channels and exocytosis and suggest that compounds that, unlike repaglinide, have direct stimulatory effects on exocytosis in somatotrophs and alpha- and beta-cells, such as sulphonylureas and nateglinide, may have a clinically undesirable general stimulatory effect on cells within the endocrine system.
AB - To investigate the hormonal and cellular selectivity of the prandial glucose regulators, we have undertaken a series of experiments, in which we characterised the effects of repaglinide and nateglinide on ATP-sensitive potassium ion (KATP) channel activity, membrane potential and exocytosis in rat pancreatic alpha-cells and somatotrophs. We found a pharmacological dissociation between the actions on KATP channels and exocytosis and suggest that compounds that, unlike repaglinide, have direct stimulatory effects on exocytosis in somatotrophs and alpha- and beta-cells, such as sulphonylureas and nateglinide, may have a clinically undesirable general stimulatory effect on cells within the endocrine system.
KW - Animals
KW - Carbamates/pharmacology
KW - Cyclohexanes/pharmacology
KW - Electrophysiology
KW - Exocytosis/drug effects
KW - Hypoglycemic Agents/pharmacology
KW - Islets of Langerhans/cytology
KW - Membrane Potentials/drug effects
KW - Nateglinide
KW - Phenylalanine/analogs & derivatives
KW - Piperidines/pharmacology
KW - Postprandial Period
KW - Potassium Channels/drug effects
KW - Rats
M3 - Journal article
C2 - 12702003
SN - 0394-3402
VL - 15
SP - 15
EP - 18
JO - Diabetes, Nutrition and Metabolism - Clinical and Experimental
JF - Diabetes, Nutrition and Metabolism - Clinical and Experimental
IS - 6 Suppl
ER -