Repaglinide at a cellular level

M Krogsgaard Thomsen; K Bokvist; M Høy; K Buschard; J J Holst; P Lindström; J Gromada

Repaglinide at a cellular level

M Krogsgaard Thomsen, K Bokvist, M Høy, K Buschard, J J Holst, P Lindström, J Gromada

1 Citation (Scopus)

Abstract

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.

Original language	English
Journal	Diabetes, Nutrition and Metabolism - Clinical and Experimental
Volume	15
Issue number	6 Suppl
Pages (from-to)	15-8
Number of pages	4
ISSN	0394-3402
Publication status	Published - Dec 2002
Externally published	Yes

Keywords

Animals
Carbamates/pharmacology
Cyclohexanes/pharmacology
Electrophysiology
Exocytosis/drug effects
Hypoglycemic Agents/pharmacology
Islets of Langerhans/cytology
Membrane Potentials/drug effects
Nateglinide
Phenylalanine/analogs & derivatives
Piperidines/pharmacology
Postprandial Period
Potassium Channels/drug effects
Rats

Cite this

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title = "Repaglinide at a cellular level",

abstract = "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.",

keywords = "Animals, Carbamates/pharmacology, Cyclohexanes/pharmacology, Electrophysiology, Exocytosis/drug effects, Hypoglycemic Agents/pharmacology, Islets of Langerhans/cytology, Membrane Potentials/drug effects, Nateglinide, Phenylalanine/analogs \& derivatives, Piperidines/pharmacology, Postprandial Period, Potassium Channels/drug effects, Rats",

author = "\{Krogsgaard Thomsen\}, M and K Bokvist and M H{\o}y and K Buschard and Holst, \{J J\} and P Lindstr{\"o}m and J Gromada",

year = "2002",

month = dec,

language = "English",

volume = "15",

pages = "15--8",

journal = "Diabetes, Nutrition and Metabolism - Clinical and Experimental",

issn = "0394-3402",

publisher = "Editrice Kurtis s.r.l.",

number = "6 Suppl",

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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

UR - https://www.scopus.com/pages/publications/0141560668

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 -

Repaglinide at a cellular level

Abstract

Keywords

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