Cited by 81Pancreatic function and diabetesIon channel regulation and functionDiabetes Treatment and Management

Differential interaction of glimepiride and glibenclamide with the β-cell sulfonylurea receptor I. Binding characteristics

Müller, Günter, Hartz, Detlev, Pünter, Jürgen, Ökonomopulos, Raymond, Kramer, Werner·1994·Biochimica et Biophysica Acta (BBA) - Biomembranes

Abstract

Glimepiride is a novel sulfonylurea drug for treatment of non-insulin-dependent diabetes mellitus with higher blood sugar lowering efficacy in diabetic patients than glibenclamide raising the question whether this characteristics is in line with different binding of glimepiride and glibenclamide to the beta-cell sulfonylurea receptor. Scatchard plot analysis of [3H]sulfonylurea binding to membranes isolated from rat beta-cell tumors and (RINm5F) insulinoma cells and to RINm5F cells demonstrated that glimepiride has a 2.5-3-fold lower affinity than glibenclamide. This corresponded well to the 8-9-fold higher koff and 2.5-3-fold higher kon rates of glimepiride compared to glibenclamide as revealed by the dissociation and association kinetics of [3H]sulfonylurea binding and the Kd values calculated thereof. In agreement, the concentrations required for half-maximal displacement of [3H]sulfonylurea bound to beta-cell membranes were significantly higher for glimepiride compared to glibenclamide. However, the binding affinity of glimepiride measured by both equilibrium binding and kinetic binding studies upon solubilization of beta-cell tumor membranes and RINm5F cell membranes increased up to the value for glibenclamide. This was primarily based on a drastic decrease of the dissociation rate constant of glimepiride whereas the kinetics of glibenclamide binding remained largely unaffected upon solubilization. These data suggest that the Kd value alone is not sufficient for characterization of a sulfonylurea drug, since the kinetic binding parameters may also determine its acute blood sugar lowering efficacy.

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  • Glimepiride, a long-acting sulfonylurea, may partly fulfil the role of a sulfonylurea with good glycemic control and low risk of hypoglycemia as it has a lower affinity for the β-cell receptor than glyburide, and its insulin secretory capacity is lower in both the fasting and postprandial states.

    “Glimepiride, a long-acting sulfonylurea, may partly fulfil this role as it has a lower affinity for the ␤-cell receptor than glyburide (117), and its insulin secretory capacity is lower in both the fasting (118) and postprandial (119) states.”

    From Hypoglycemia in Type 2 Diabetes (2005) · cites this paper as [117]

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Research works printed but not linked: 1

  1. [22][22] Chick, W.L., Warren, S., Chute, R.N., Like, N.A., Lauris, V. and Kitchen, K. (1977) Proc. Natl. Acad. Soc. USA 74, 628–632. -

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Authors
Müller, G., Hartz, D., Pünter, J., Ökonomopulos, R., & Kramer, W.
Corresponding author
Müller, Günter
Venue
Biochimica et Biophysica Acta (BBA) - Biomembranes
Publisher
Elsevier BV
Published
1994-05
Volume
1191
Issue
2
Pages
267-277
ISSN
0005-2736 (ISSN-L)
OpenAlex
W2158049984
Cited by
81
References
33
Citations by year
2025: 1 · 2023: 1 · 2022: 2 · 2018: 1 · 2016: 3 · 2015: 5 · 2014: 3 · 2013: 4 · 2012: 5
FWCI
5.49
Type
journal article
Language
en
Open access
closed
Locations
  • Biochimica et Biophysica Acta (BBA) - Biomembranes (publishedVersion)
  • PubMed (publishedVersion)
  • Open access LMU (Ludwid Maxmilian's Universitat Munchen) (submittedVersion)
Topics
  • Health Sciences › Medicine › Surgery › Pancreatic function and diabetes
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
Keywords
glimepiride, glibenclamide, sulfonylurea receptor, SUR1, binding kinetics, dissociation rate constant, association rate constant, type 2 diabetes
MeSH terms
Animals, Cell Line, Cell Membrane, Diabetes Mellitus, Type 2, Glyburide, Hypoglycemic Agents, Kinetics, Pancreas, Receptors, Drug, Sulfonylurea Compounds, Tritium, Potassium Channels, ATP-Binding Cassette Transporters, Potassium Channels, Inwardly Rectifying, Rats, Sulfonylurea Receptors

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