drug metabolite

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.

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

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.

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

(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.

3-Sulfopropanoic acid, a major metabolite of treprostinil and its prodrug ALZ-801, is an endogenous molecule present in the cerebrospinal fluid (CSF) of AD patients that inhibits the formation of Aβ42 oligomers.

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.

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

Gentisuric acid, an Aspirin metabolite and a substrate of α-amidating monooxygenase (PAM), mitigates DNA damage induced by Mitomycin C. [1] [2]

Deslanoside (Desacetyllanatoside C) is a rapidly acting cardiac glycoside used to treat congestive heart failure and supraventricular arrhythmias associated with reentry mechanisms. It inhibits the Na-K-ATPase membrane pump, increasing intracellular sodium and calcium concentrations.

Perindopril acyl-β-D-glucuronide is a metabolite of the ACE inhibitor perindopril [1].

RPR132595A (NPC) hydrochloride, an active metabolite of CPT-11, is produced via cytochrome P-450 3A4 (CYP3A4) metabolism and is ultimately eliminated via urinary excretion [1].

3-Hydroxycarbofuran, a principal metabolite of Carbofuran, acts as a reversible inhibitor of acetylcholinesterase (AChE) [1].

(R)-tert-OMe-byakangelicin, a furanocoumarin, exhibits inhibitory effects on liver drug metabolizing enzyme (DME) activity and can be isolated from the immature fruits of Angelica sinensis [1] [2].

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

N-Methyl Palbociclib is an impurity of the orally active, selective CDK4 and CDK6 inhibitor Palbociclib (PD 0332991).

Compound 5, DDC 3′-O-β-D-glucuronide, is a drug metabolite with properties that inhibit the fibrillization and oligomerization of Aβ42, suggesting its potential utility in Alzheimer's disease research [1].

2-Phenyl-2-(2-pyridyl)acetonitrile is the principal metabolite of the antigastric agent SC 15396, produced by the supernatant fraction of rat liver homogenate. SC 15396 inhibits gastric secretion [1].

Homoeriodictyol, a naturally occurring, bitter-masking flavanone, as a promising agent to increase appetite and food intake. The flavanone homoeriodictyol can increase SGLT-1-mediated glucose uptake but decrease serotonin release in differentiated Caco-2 cells.

2′,2′-Difluorodeoxyuridine (dFdU), the major metabolite of Gemcitabine, exhibits anticancer and antitumor activities, shows radiosensitization under hypoxic conditions, and can be used to study pancreatic cancer.

Quercetin 7-glucuronide (Quercetin 7-O-β-glucuronide), a Quercetin metabolite found in Madagascarian Uncarina species, inhibits LDL oxidation [1].

GS-829845 is a JAK1 inhibitor, the main component of the active metabolite of Filgotinib, which is approximately 10-fold less potent and has a longer half-life than the parent.

DP-1 hydrochloride is a degradation product of SDC-TRAP-0063, a fragment of Ganetespib, a heat shock protein 90 (HSP90) inhibitor with antitumor activity.