1. Novel Partial Agonist of PPAR-Gamma for Treatment of Diabetic Neuropathy in Rats
- Author
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Daniel N. do Amaral, Jaqueline S da Silva, Lídia Moreira Lima, Josenildo S Araujo, Eliezer J. Barreiro, Roberto T. Sudo, Gisele Zapata-Sudo, and Margarete M. Trachez
- Subjects
Agonist ,medicine.medical_specialty ,Triglyceride ,business.industry ,medicine.drug_class ,Insulin ,medicine.medical_treatment ,Analgesic ,medicine.disease ,Streptozotocin ,Partial agonist ,chemistry.chemical_compound ,Endocrinology ,chemistry ,Diabetes mellitus ,Internal medicine ,Hyperalgesia ,Medicine ,medicine.symptom ,business ,medicine.drug - Abstract
This work describes a novel ligand for peroxisome proliferator-activated receptor gamma (PPARgamma) and its hypoglycemic and analgesic activity in a murine model of diabetes-induced neuropathic pain. The molecular recognition of LASSBio-1772 by a PPARgamma binding domain showed that the compound is a partial agonist. Four weeks after male Wistar rats received a single intravenous injection of streptozotocin (STZ, 60 mg/kg), plasma glucose levels were increased from 92.5 ± 3.7 to 465.0 ± 21.6 mg/dL (P < 0.01) and serum insulin was reduced from 66.8 ± 7.8 to 25.5 ± 5.6 pmol/L (P
- Published
- 2014
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