Cytochrome P450 2D6 (CYP2D6) Inhibitor Screening Kit (Fluorometric)

Cytochrome P450 2D6 (CYP2D6, EC 1.14.14.1) is a member of the cytochrome P450 monooxidase (CYP) family of microsomal xenobiotic metabolism enzymes. CYPs are membrane-bound hemeproteins responsible for Phase I biotransformation reactions, in which lipophilic drugs and other xenobiotic compounds are converted to more hydrophilic products to facilitate excretion from the body. CYP2D6 catalyzes oxidation of lipophilic bases with an aromatic ring and a nitrogen atom and is highly expressed in liver and brain tissue. The enzyme is responsible for metabolism of nearly 25% of all small molecule drugs commonly used by humans, particularly psychiatric drugs such as antidepressants, antipsychotics and stimulants. The CYP2D6 gene is highly polymorphic in the human population, with resulting CYP2D6 activity ranging from complete metabolic deficiency to ultra-rapid metabolism depending upon allelic variation and gene copy number. Due to this wide phenotypic variability, CYP2D6 is frequently implicated in drug toxicity and clinical drug/drug interactions. In addition, for drugs whose pharmacological activity requires metabolism from a pro-drug form, CYP2D6 inhibition or allelic deficiency can lead to decreased drug efficacy. BioVision’s CYP2D6 Inhibitor Screening Kit enables rapid screening of drugs and other new chemical entities (NCEs) for compound-CYP2D6 interaction in a reliable, high-throughput fluorescence-based assay. The kit provides a yeast microsomal preparation of human CYP2D6 and cytochrome P450 reductase (CPR) enzymes. The assay utilizes a non-fluorescent CYP2D6-selective substrate that is converted into a highly fluorescent metabolite detected in the visible range (Ex/Em = 390/468 nm), ensuring a high signal-to-background ratio with little interference by autofluorescence. The kit contains a complete set of reagents sufficient for performing 200 reactions in a 96-well plate format.