drugmetabolite

Clozapine N-oxide is the major metabolite of Clozapine and is blood-brain barrier permeable. Clozapine N-oxide is an agonist of DREADDs and activates the DREADD receptors hM3Dq and hM4Di. Clozapine N-oxide is also a dopamine antagonist and selective muscarinic M4 receptor agonist.

4-Hydroxymephenytoin ((+ -)-4'-Hydroxymephenytoin) is the metabolism of an antiepileptic drug mephenytoin. Mephenytoin is used as a CYP2C19 substrate.

Leukotriene D4 (LTD4) is a potent pro-inflammatory mediator formed from arachidonic acid, a bronchoconstrictor, and induces osteoclast senescence.Leukotriene D4 induces transcriptional activity of potentially oncogenic genes and can be used in the study of asthma.

2-Hydroxy atorvastatin calcium salt is a hydroxy metabolite of atorvastatin calcium salt, a potent HMG-CoA reductase inhibitor (IC50 = 8 nM).

Monobutyl phthalate, the main metabolite of dibutyl phthalate, is an embryotoxin with antiandrogenic properties.

Nicotinamide N-oxide (Nicotinamide 1-oxide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. The enzyme that catalyzes the reduction of nicotinamide N-oxide to nicotinamide in the liver is xanthine oxidase.

p-Coumaric Acid Ethyl Ester (Ethyl (E)-p-hydroxycinnamate) is the ethyl ester of p-Coumaric acid. p-Coumaric Acid is a common dietary polyphenol and also a potent immunosuppressive agent in treating autoimmune inflammatory diseases like rheumatoid arthritis.

Dimetridazole is a nitroimidazole-based compound with antibacterial and anticoccidial activity. It was once widely used in the treatment of parasitic infections in poultry, cattle, swine and farmed fish until suspected to be carcinogenic and mutagenic to humans. Hydroxy dimetridazole is a metabolite of dimetridazole that may be useful for identifying this nitroimidazole in various agricultural samples through liquid chromatography-tandem mass spectrometry and other methods.

3-Methoxytyramine hydrochloride (3-O-methyl Dopamine hydrochloride) is an inactive metabolite of dopamine which can activate trace amine associated receptor 1 (TAAR1). 3-methoxytyramine can be found primarily in human brain and most tissues tissues; and in blood, cerebrospinal fluid (csf) or urine. Within a cell, 3-methoxytyramine is primarily located in the cytoplasm.

Tulipalin A (α-methylene-γ-butyrolactone) (2-Methylenebutyrolactone) which has some phytotoxicity is a natural compound extracted from Tulipa gesneriana.

Mycophenolate Mofetil (TM-MMF), an immunosuppressive agent, is the 2-morpholinoethyl ester of mycophenolic acid (MPA), and an inhibitor of inosine monophosphate dehydrogenase (IMPDH).

4-(4-Amino-3-fluorophenoxy)-N-methylpicolinamide is an aromatic enigma that is is a metabolite of the antitumor drug rafenil.

Homovanillyl alcohol, a biological metabolite of Hydroxytyrosol, is a phenolic compound found in virgin olive oil (VOO) and wine. It exhibits high scavenging activities, protects red blood cells from hemolysis in a dose-dependent manner, and has a protective effect on cardiovascular disease and total mortality.

Norgestimate metabolite Norelgestromin (17-Deacylnorgestimate) is one of the active metabolites of norgestimate.It is a steroidal progestin used in contraceptive patches, where it is combined with the estrogen ethinyl estradiol.

4-Methylamino antipyrine, an active metabolite of Metamizole, a pyrazolone non-steroidal anti-inflammatory drug (NSAID) that inhibits COX, possesses analgesic, antipyretic, and relatively weak anti-inflammatory properties.

CNDAC hydrochloride, a nucleoside analog, is a metabolite of the sapacitabine.

Vinburnine (Eburnalritardo) is a vasodilator. Vinburnine is a vinca alkaloid and a metabolite of vincamine.

Etilevodopa hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.

4-hydroperoxy cyclophosphamide (4-OOH-CY) is an active metabolite of Cyclophosphamide that induces hepatotoxicity.4-Hydroperoxy cyclophosphamide increases levels of glutaminase and aspartate aminotransferase, enhances inflammatory factors and oxidative markers, and Inhibits oxidoreductase activity.4-Hydroperoxy cyclophosphamide is used in the study of cancer and autoimmune diseases.

6α-hydroxy Paclitaxel (6α-OH-PTX) is a major metabolite of the anticancer compound paclitaxel and is partially cytotoxic.

Phosphoramide mustard is a toxic metabolite of cyclophosphamide with anticancer activity and ovarian toxicity that induces DNA damage.

Monoethyl phthalate, a metabolite of diethyl phthalate, serves as a urinary biomarker for phthalate exposure and indicates potential risks of thyroid cancer and benign nodules.

(±)-Equol ((R,S)-Equol) is a non-steroidal estrogen produced from the metabolism of the isoflavonoid phytoestrogen daidzen by human intestinal microflora. The estrogen receptor (ER) agonist activity of the naturally occurring (S)-enantiomer (EC50 = 85 and 65 nM for human ERα and ERβ, respectively) is similar to that of genistein but exceeds that of daidzein. (±)-Equol preferentially binds ERβ (Ki = 0.73 nM) and demonstrates approximately 9-fold lower affinity for ERα (Ki = 6.41 nM). (±)-Equol is also a potent antagonist of dihydrotestosterone, which has important implications for prostate cancer and other androgen-mediated pathologies.

(E Z)-Endoxifen ((E Z)-Endoxifen) is an active metabolite of tamoxifen produced by the sequential action of cytochrome P450 (CYP) isoforms, including CYP2D6. It is a strong anti-estrogen, as it has an approximately 100-fold greater affinity for estrogen receptors than tamoxifen. As the efficient conversion of tamoxifen to endoxifen depends on CYP2D6, polymorphisms in this CYP isoform can impact the effectiveness of TMX treatment.