Rosiglitazone is a member of the thiazolidinedione class of drugs.
Thiazolidinediones act as insulin sensitizers.
They reduce glucose, fatty acid, and insulin blood concentrations.
They work by binding to the peroxisome proliferator-activated receptors (PPARs).
PPARs are transcription factors that reside in the nucleus and become activated by ligands such as thiazolidinediones.
Thiazolidinediones enter the cell, bind to the nuclear receptors, and alter the expression of genes.
The several PPARs include PPARα, PPARβ/δ, and PPARγ.
Thiazolidinediones bind to PPARγ.

PPARs are expressed in fat cells, cells of the liver, muscle, heart, and inner wall (endothelium) and smooth muscle of blood vessels.
PPARγ is expressed mainly in fat tissue, where it regulates genes involved in fat cell (adipocyte) differentiation, fatty acid uptake and storage, and glucose uptake.
It is also found in pancreatic beta cells, vascular endothelium, and macrophages Rosiglitazone is a selective ligand of PPARγ and has no PPARα-binding action.
Other drugs bind to PPARα.

Rosiglitazone also appears to have an anti-inflammatory effect in addition to its effect on insulin resistance.
Nuclear factor kappa-B (NF-κB), a signaling molecule, stimulates the inflammatory pathways.
NF-κB inhibitor (IκB) downregulates the inflammatory pathways.
When patients take rosiglitazone, NF-κB levels fall and IκB levels increase.
Rosiglitazone is a member of the thiazolidinedione class of drugs. Thiazolidinediones act as insulin sensitizers. They reduce glucose, fatty acid, and insulin blood concentrations. They work by binding to the peroxisome proliferator-activated receptors (PPARs). PPARs are transcription factors that reside in the nucleus and become activated by ligands such as thiazolidinediones. Thiazolidinediones enter the cell, bind to the nuclear receptors, and alter the expression of genes. The several PPARs include PPARα, PPARβ/δ, and PPARγ. Thiazolidinediones bind to PPARγ.
PPARs are expressed in fat cells, cells of the liver, muscle, heart, and inner wall (endothelium) and smooth muscle of blood vessels. PPARγ is expressed mainly in fat tissue, where it regulates genes involved in fat cell (adipocyte) differentiation, fatty acid uptake and storage, and glucose uptake. It is also found in pancreatic beta cells, vascular endothelium, and macrophages Rosiglitazone is a selective ligand of PPARγ and has no PPARα-binding action. Other drugs bind to PPARα.
Rosiglitazone also appears to have an anti-inflammatory effect in addition to its effect on insulin resistance. Nuclear factor kappa-B (NF-κB), a signaling molecule, stimulates the inflammatory pathways. NF-κB inhibitor (IκB) downregulates the inflammatory pathways. When patients take rosiglitazone, NF-κB levels fall and IκB levels increase.
Rosiglitazone