CITCO (drug)

{{Drugbox | Verifiedfields = changed | verifiedrevid = 477241123 | IUPAC_name = 2-[[3-(1,3-Benzodioxol-5-yl)-2-methylpropyl]amino]-1,2-diphenylethanol | image = CITCO_structure.png | width = 200 | CAS_number = 160939-09-3 | PubChem = 5311450 | ChemSpiderID = 4470915 | UNII = 0A9T0B5YI9 | KEGG = D08895 | ChEMBL = 109694 | C=25 | H=25 | N=1 | O=3 | smiles = CC(Cc1ccc2c(c1)OCO2)NCC(C3=CC=CC=C3)C4=CC=CC=C4O }}

CITCO (6-(4-Chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oxime) is a synthetic chemical compound that acts as a potent and selective agonist of the Constitutive Androstane Receptor (CAR), a nuclear receptor that regulates the expression of genes involved in drug metabolism and clearance.

Mechanism of Action

CITCO functions by binding to the Constitutive Androstane Receptor (CAR), which is a member of the nuclear receptor superfamily. CAR is primarily expressed in the liver and plays a crucial role in the regulation of genes involved in xenobiotic metabolism, including the Cytochrome P450 family of enzymes. Upon activation by CITCO, CAR translocates to the nucleus where it binds to specific response elements in the DNA, leading to the transcriptional activation of target genes.

Pharmacological Effects

The activation of CAR by CITCO results in the induction of various Cytochrome P450 enzymes, such as CYP2B6 and CYP3A4, which are involved in the metabolism of a wide range of drugs and endogenous compounds. This can lead to increased clearance of drugs that are substrates for these enzymes, potentially affecting their pharmacokinetics and therapeutic efficacy.

Research and Applications

CITCO is primarily used as a research tool to study the function of CAR and its role in drug metabolism and detoxification processes. It has been instrumental in elucidating the pathways and regulatory mechanisms controlled by CAR, providing insights into how drugs and other xenobiotics are processed by the body.

Safety and Toxicity

As a research chemical, CITCO is not intended for human or veterinary use. Its safety profile has not been extensively studied, and it should be handled with caution in laboratory settings.

Also see

• Constitutive Androstane Receptor
• Cytochrome P450
• Nuclear Receptor
• Drug Metabolism