monooxygenase

3-Hydroxyphenylacetic acid is a rutin metabolite and an antioxidant. It has a protective biological activity in human. It is a substrate of enzyme 4-hydroxyphenylacetate 3-monooxygenase [EC 1.14.13.3] in the pathway tyrosine metabolism. 3-Hydroxyphenylace

Thiacetazone (Diazam) is a thiosemicarbazone that thioacetazone treatment of pulmonary tuberculosis

Diallyl disulfide has antitumor effect, the effect can be enhanced by miR-200b and miR-22.

Zamicastat (BIA 5-1058) is an inhibitor of dopamine β-hydroxylase (DBH) and a concentration-dependent dual inhibitor of P-gp and BCRP, with IC50 values of 73.8 μM and 17.0 μM, respectively.

Guanoclor (VATENSOL) (INN), also known as guanochlor, is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.

1-Phenylpyrrole (NSC-16581) is an inhibitor of CYP450 dependant monooxygenase activity in microsomes from rat liver.

Racemetirosine is an inhibitor of Tyrosine 3-monooxygenase, and consequently it inhibits the synthesis of catecholamines.

Metyrapone (NSC-25265) is an inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.

Metyrapone Tartrate is an inhibitor of the STEROID 11-beta-monooxygenase enzyme which is used as a test for feedback hypothalamic-pituitary mechanism in the diagnosis of Cushing SYNDROME.

GSK 366 is a potent kynurenine-3-monooxygenase (KMO) inhibitor with IC50 values of 0.7 nM for P. fluorescens-KMO and 2.3 nM for human KMO.

Isoasatone A, a natural product isolated from the plant [Heterotropa takaoi M.], exhibits anti-insect activity.

UPF-648 sodium salt is an inhibitor of kynurenine 3-monooxygenase (KMO) and exhibits highly active at 1 uM (81 ± 10% KMO inhibition).

UPF-648 is a potent kynurenine 3-monooxygenase (KMO) inhibitor, demonstrating high activity at 1 µM with 81 ± 10% inhibition.

Cevimeline hydrochloride hemihydrate ((-)-SNI-2011), a novel muscarinic receptor agonist, is being explored as a potential treatment for xerostomia in Sjogren's syndrome, exhibiting an IC50 value indicative of its affinity for mAChR. This compound's pharmacological effects on the gastrointestinal, urinary, and reproductive systems, alongside its impact on various tissues, were thoroughly examined in species including mice, rats, guinea pigs, rabbits, and dogs. The metabolic breakdown of (-)-SNI-2011 was studied in vitro using rat and dog liver microsomes to assess its biotransformation. Upon oral administration, peak plasma concentrations were reached within an hour in both rats and dogs, showcasing rapid absorption and a subsequent decrease in concentration with a half-life ranging from 0.4 to 1.1 hours. Bioavailability was noted at 50% in rats and 30% in dogs. Metabolic pathways highlighted significant species differences, with both S- and N-oxidized metabolites identified in rats, but only N-oxidized metabolites in dogs. Additionally, gender differences in pharmacokinetics were observed in rats but were absent in dogs. In vitro studies pinpointed the involvement of cytochrome P450 (CYP) and flavin-containing monooxygenase (FMO) in the metabolism of (-)-SNI-2011, specifically through sulfoxidation and N-oxidation processes, respectively. CYP2D and CYP3A were identified as the primary enzymes responsible for sulfoxidation in rat liver microsomes.

(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011), a potent muscarinic receptor agonist, shows promise as a therapeutic candidate for xerostomia in Sjogren's syndrome. It exhibits a broad pharmacological profile across various systems in animal models including mice, rats, guinea pigs, rabbits, and dogs. Metabolism studies using rat and dog liver microsomes reveal rapid absorption with peak plasma concentrations (Cmax) within one hour post-oral administration and a half-life (t1 2) between 0.4 to 1.1 hours. Bioavailability is 50% in rats and 30% in dogs. Metabolic analysis shows species-specific differences: rats produce S- and N-oxidized metabolites, while dogs produce only N-oxidized metabolites. Sex-based pharmacokinetic differences were noted in rats but not in dogs. In vitro studies indicate cytochrome P450 (CYP) and flavin-containing monooxygenase (FMO) involvement in the sulfoxidation and N-oxidation of SNI-2011, with CYP2D and CYP3A mainly responsible for sulfoxidation in rat liver microsomes.

GSK180 is a selective competitive inhibitor of kynurenine 3-monooxygenase (KMO; IC50: ~6 nM), an enzyme involved in tryptophan metabolism.

NSC-152035 is an inhibitor of tyrosine 3-monooxygenase.

Licodione is a Cytochrome P450 Monooxygenase Catalyzing 2-Hydroxylation of 5-Deoxyflavanone.

5-hydroxy Omeprazole is a major metabolite of omeprazole , an inhibitor of the gastric H+/K+-ATPase pump.[1] 5-hydroxy Omeprazole is produced from omeprazole by the action of cytochrome P450 (CYP) isoform 2C19, a monooxygenase. [2][3] CYP2C19 polymorphisms significantly influence the metabolism of omeprazole, and individuals may be classified as homozygous extensive metabolizers, heterozygous extensive metabolizers, and poor metabolizers.[1]

JM6 is a weak kynurenine 3-monooxygenase (KMO) inhibitor that targets mouse KMO (IC50: 19.85 μM) and can be used to study Alzheimer's disease.

Nepicastat hydrochloride (RS-25560-197 hydrochloride) is an effective and specific inhibitor, which is used for bovine and human dopamine-β-hydroxylase with IC50 of 8.5 nM and 9 nM, respectively.The affinity of Nepicastat for twelve other enzymes and thirteen neurotransmitter receptors is negligible.

Hypericin (Cyclosan) is a natural anthraquinone compound, an extract of Hypericum perforatum, which inhibits PKC, MAO, dopamine-beta-hydroxylase, reverse transcriptase, telomerase, and CYP, etc. Hypericin exhibits antimicrobial, antiviral, antitumor, and antidepressant activities.

GSK065 is a potent inhibitor of kynurenine-3-monooxygenase (KMO).

Benzydamine N-Oxide, a metabolite of Benzydamine, serves as a biomarker for flavin-containing monooxygenase activity [1] [2].