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Sulfonylurea receptors and mechanism of sulfonylurea action

Experimental and Clinical Endocrinology & Diabetes, 2009
Binding of hypoglycemic sulfonylureas and their analogues to the sulfonylurea receptor in the beta-cell plasma membrane mediates closure of the ATP-sensitive K+-channel (KATP-channel) and thereby stimulation of insulin release. The sulfonylurea receptor is a member of the traffic ATPase family with two intracellular nucleotide binding folds.
U, Panten   +2 more
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SULFONYLUREAS

Endocrinology and Metabolism Clinics of North America, 1997
Sulfonylureas have been available for the treatment of non-insulin-dependent diabetes mellitus (NIDDM) since the 1950s. With the introduction of new oral agents, there is a tendency to discount the value of sulfonylurea therapy. Sulfonylureas have the advantage of multiple formulations, low costs, minimal side effects, and demonstrated efficacy in ...
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Potential Hypoglycemic Sulfonylureas

Journal of Pharmaceutical Sciences, 1964
A series of N ′-alkyl- N - p -phenylbenzenesulfonylureas and N , N ′-bis ( N -alkylcarbamyl) 4,4′-biphenyldisulfonamides has been prepared for pharmacological studies of their hypoglycemic activities.
K A, NIEFORTH, G L, JENKINS, A M, KNEVEL
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Sulfonylureas

Reactions Weekly, 1990
Oral antidiabetics are an important aspect of treatment in many diabetics and in the last few years with new developments in the knowledge of type II diabetes physiopathology, there has been a lot of interest in their actions mechanisms. Oral therapy is nevertheless a mere complement which needs to be fitted into a wider group of measures: diabetics ...
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Sulfonylureas in NIDDM

Diabetes Care, 1992
Sulfonylureas have represented the backbone of oral therapy in non-insulin-dependent diabetes mellitus for > 30 yr. Despite this, our knowledge about the mode of actions of these agents is limited, and the use of them is far from rational. Sulfonylureas lower blood glucose concentrations primarily by stimulating insulin secretion.
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Sulfonylureas

Sulfonylureas have been a mainstay in the pharmacologic treatment of T2D for over 60 years. The first-generation sulfonylureas (e.g., chlorpropamide, tolbutamide, and tolazamide) are no longer available in the United States. With the availability of many noninsulin classes of medications for T2D, sulfonylurea usage is on the decline, yet their use ...
Elmo M. Beyer   +3 more
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Sulfonylurea Signal Transduction

1991
In the pancreatic beta cells the proximal step in sulfonylurea signal transduction is the binding of these clinically important drugs to high-affinity receptors in the beta cell membrane. Using HIT cells as a model system, we have established an extremely close correlation between the affinity of binding of glyburide and its analog, iodoglyburide, and ...
A E, Boyd   +9 more
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Hyperlipemia and Sulfonylurea Therapy

JAMA, 1964
To the Editor:— A report by Shipp et al ( JAMA 188: 468 [May 4] 1964), describing severe hyperlipemia in three diabetics treated with sulfonylurea compounds, proposes that "... enough control to prevent ketosis, but not enough to prevent hyperglycemia, may have provided a longterm metabolic balance favoring the development of hyperlipemia." It is ...
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Management of sulfonylurea ingestions

Pediatric Emergency Care, 1999
In the majority of pediatric patients with an unintentional ingestion of a sulfonylurea, observation and, if necessary, intravenous glucose supplementation, are sufficient. However, with cases of persistent hypoglycemia or cases refractory to IV glucose supplementation, attempts to inhibit insulin secretion should be considered.
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Rational use of sulfonylureas

Postgraduate Medicine, 1992
The clinical use of sulfonylureas described in this article is both rational and effective for diabetic patients. Sulfonylureas are not used (1) in patients with insulin-dependent (type I) diabetes, because they are completely ineffective or (2) in patients with non-insulin-dependent (type II) diabetes who respond satisfactorily to diet, because they ...
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