Cytochrome P450 inhibitors

Cimetidine, sold under the brand name Tagamet among others, is a histamine H2 receptor antagonist that inhibits stomach acid production. It is mainly used in the treatment of heartburn and peptic ulcers.

Dihydromethysticin is one of the six major kavalactones found in the kava plant. It is known for its anxiolytic, analgesic, and anticonvulsant properties. It induces the liver enzymes CYP1A1 and CYP3A through mechanisms involving the aryl hydrocarbon receptor and potentially pregnane X receptor-independent transcriptional activation. Dihydromethysticin acts synergistically with other kavalactones, modulates NMDA receptors and voltage-dependent calcium channels, and functions as a GABAA receptor positive allosteric modulator and monoamine oxidase B inhibitor. Dihydromethysticin shows high syste

Amentoflavone is a biflavonoid (bis-apigenin coupled at 8 and 3 positions, or 3,8-biapigenin) constituent of a number of plants including Ginkgo biloba, Chamaecyparis obtusa (hinoki), Biophytum sensitivum, Selaginella tamariscina, Hypericum perforatum (St. John's Wort) and Xerophyta plicata.

ε-Viniferin is a naturally occurring polyphenol, belonging to the stilbenoids family. It is a resveratrol dimer.

Rhapontigenin is a stilbenoid. It can be isolated from Vitis coignetiae or from Gnetum cleistostachyum.

Proadifen (SKF-525A) is a non-selective inhibitor of cytochrome P450 enzymes, preventing some types of drug metabolism. It is also an inhibitor of neuronal nitric oxide synthase (NOS), CYP-dependent (cytochrome P450-dependent) arachidonate metabolism, transmembrane calcium influx, and platelet thromboxane synthesis. Further documented effects include the blockade of ATP-sensitive inward rectifier potassium channel 8 (KIR6.1), and stimulation of endothelial cell prostacyclin production.