O-Desmethyl metoprolol, a metabolite of metoprolol, acts as a β1-adrenergic receptor (β1-AR) antagonist. This compound is produced through the metabolism of metoprolol by the cytochrome P450 (CYP) isoform CYP2D6.
O-Desmethyl-N-deschlorobenzoyl indomethacin is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor indomethacin .1It is formed from indomethacin in isolated rabbit hepatocytes. O-Desmethyl-N-deschlorobenzoyl indomethacin (600 μM) decreases the viability of HL-60 leukemia cells when cultured with glucose oxidase.2It has also been used in the synthesis of prostaglandin D2receptor antagonists.3 1.Evans, M.A., Papazafiratou, C., Bhat, R., et al.Indomethacin metabolism in isolated neonatal and fetal rabbit hepatocytesPediatr. Res.15(11)1406-1410(1981) 2.Morgan, A.G.M., Babu, D., Michail, K., et al.An evaluation of myeloperoxidase-mediated bio-activation of NSAIDs in promyelocytic leukemia (HL-60) cells for potential cytotoxic selectivityToxicol. Lett.28048-56(2017) 3.Torisu, K., Kobayashi, K., Iwahashi, M., et al.Discovery of new chemical leads for prostaglandin D2 receptor antagonistsBioorg. Med. Chem. Lett.14(17)4557-4562(2004)
O-desmethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1,2It inhibits CAII and CAIV (IC50s = 0.136 and 165 nM, respectively).1 1.Huang, Q., Rui, E.Y., Cobbs, M., et al.Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressureJ. Med. Chem.58(6)2821-2833(2015) 2.Lo Faro, A.F., Tini, A., Gottardi, M., et al.Development and validation of a fast ultra-high-performance liquid chromatography tandem mass spectrometry method for determining carbonic anhydrase inhibitors and their metabolites in urine and hairDrug Test Anal.13(8)1552-1560(2021)
Mebeverine metabolite O-desmethyl Mebeverine alcohol is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract. Mebeverine metabolite O-desmethyl Mebeverine alcohol is a metabolite of Mebeverine.
Taurocholic acid 3-sulfate (TCA3S) is a metabolite of the conjugated bile acid taurocholic acid .1Plasma levels of TCA3S are elevated in wild-type andSortilin 1(Sort1) knockout mice at 6 hours following bile duct ligation (BDL) and are further elevated inSort1knockout mice at 24 hours post-BDL.2 1.Lefebvre, P., Cariou, B., Lien, F., et al.Role of bile acids and bile acid receptors in metabolic regulationPhysiol. Rev.89(1)147-191(2009) 2.Li, J., Woolbright, B.L., Zhao, W., et al.Sortilin 1 loss-of-function protects against cholestatic liver injury by attenuating hepatic bile acid accumulation in bile duct ligated miceToxicol. Sci.161(1)34-47(2018)
o-Iodohippurate sodium is an analogue of p-aminohippuric acid used to determine effective renal plasma flow. Labelled OIH has a higher clearance than other radiopharmaceutical yet developed and is extremely suitable for renography. It is eliminated mainly
Prasterone is an endogenous steroid hormone. Prasterone acts as an agonist at ERβ, NMDA, and σ1 receptors, a partial agonist at ERα and AR, and antagonist at GABA-A receptors. It displays a variety of biologocial activities, including enhancing working me
Taurolithocholic acid 3-sulfate (TLCA3S) is a metabolite of the conjugated bile acid taurolithocholic acid . TLCA3S has been used to study bile acid transport in cellular models and to induce pancreatitis in mouse models of bile acid infusion pancreatitis.
6-O-desmethyl Donepezil is an active metabolite of the acetylcholinesterase inhibitor donepezil . It is formed through dealkylation by the cytochrome P450 (CYP) isoform CYP2D6. It inhibits human ether a go-go (hERG) channels (IC50 = 1.5 μM in HEK293 cells expressing hERG).
O-Desmethylapixaban is a metabolite of Apixaban and a highly selective, reversible inhibitor of Factor Xa, with Ki values of 0.08 nM in humans and 0.17 nM in rabbits.
Moxifloxacin N-sulfate is a metabolite of moxifloxacin . Moxifloxacin is a fluoroquinolone antibiotic. Formulations containing moxifloxacin have been used in the treatment of bacterial infections, including sinusitis, chronic bronchitis, and pneumonia.
Aldosterone 21-sulfate is a metabolite of the steroid hormone aldosterone .1It reduces the sodium-to-potassium ratio in rat urine when administered at doses ranging from 10 to 100 μg, indicating mineralocorticoid activity that is less than 1% that of aldosterone.2 1.Grose, J.H., Nowaczynski, W., Kuchel, O., et al.Isolation of aldosterone urinary metabolites, glucuronides and sulfateJ. Steroid Biochem.4(6)551-566(1973) 2.Jowett, T.P., and Slater, J.D.H.Aldosterone 21-sulphate in manJ. Steroid. Biochem.18(4)471-479(2019)