Repaglinide at a cellular level

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

Repaglinide at a cellular level

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

Endocrinology and Metabolism

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.

Originalsprog	Engelsk
Tidsskrift	Diabetes, nutrition & metabolism
Vol/bind	15
Udgave nummer	6 Suppl
Sider (fra-til)	15-8
Antal sider	4
ISSN	0394-3402
Status	Udgivet - dec. 2002

Citationsformater

@article{6fab28d68ad4438590ce51313791323f,

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, Cyclohexanes, Electrophysiology, Exocytosis, Hypoglycemic Agents, Islets of Langerhans, Membrane Potentials, Phenylalanine, Piperidines, Postprandial Period, Potassium Channels, Rats",

author = "{Krogsgaard Thomsen}, M and K Bokvist and M H{\o}y and K Buschard and Holst, {Jens Juul} 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 = "EditriceKurtis s.r.l.",

number = "6 Suppl",

}

TY - JOUR

T1 - Repaglinide at a cellular level

AU - Krogsgaard Thomsen, M

AU - Bokvist, K

AU - Høy, M

AU - Buschard, K

AU - Holst, Jens Juul

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

KW - Cyclohexanes

KW - Electrophysiology

KW - Exocytosis

KW - Hypoglycemic Agents

KW - Islets of Langerhans

KW - Membrane Potentials

KW - Phenylalanine

KW - Piperidines

KW - Postprandial Period

KW - Potassium Channels

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 -

Repaglinide at a cellular level

Abstract

Fingeraftryk

Citationsformater