Toxicology of Sulfonylureas

Härtig, Florian; Langer, K; Rebel, W.; Schmidt, Felix; Schütz, Erich

doi:10.1007/978-3-662-09127-2_8

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Acute Toxicity1

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2015

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“…For example, Murcia-Soler et al [4] reported that tolbutamide had LD 50 = 1.27 g/kg and glibornuride had LD 50 = 5.00 g/kg, whereas Hartig et al [32] reported 467 mg/kg for tolbutamide and 1.53 g/kg for glibornuride. For consistency, we have used the values given by Murcia-Soler et al [4].…”

Section: Acute Toxicitymentioning

confidence: 97%

QSAR study of some anti-hyperglycaemic sulphonylurea drugs

Dearden

Hewitt

Rowe

2015

SAR and QSAR in Environmental Research

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Sulphonylureas are widely used anti-hyperglycaemic drugs for the treatment of type 2 diabetes. The only published quantitative structure-activity relationship (QSAR) models for sulphonylurea drugs have been found to be questionable, for a number of reasons. We have re-analysed the human anti-hyperglycaemic potencies, acute mouse intraperitoneal toxicities (LD50) and plasma protein-binding abilities of the 15 drugs using multiple linear regression and obtained good QSAR models for each endpoint. The obtained QSARs all comply well with the Organisation for Economic Co-operation and Development (OECD) Guidelines for the Validation of (Q)SARs. We could not carry out external validation of our models for acute toxicity and plasma protein-binding because of the very small datasets available.

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Section: Acute Toxicitymentioning

confidence: 97%