Bêta-bloquants

Applications A labelled nonsteroidal anti-inflammatory drug (NSAID); activity resides primarily in the (S)-isomer.
References Busson, M., et al.: J. Int. Med Res., 14, 53 (1986), Meade, E.A., et al.: J. Biol. Chem., 268, 6610 (1993), Davies, N.M., et al.: Clin. Pharmacokinet., 34, 101 (1998),

Impurity Carvedilol EP Impurity B; Carvedilol Impurity B; Carvedilol USP B
Applications Carvedilol Bis-carbazole (Carvedilol EP Impurity B; Carvedilol Impurity B; Carvedilol USP B) is an impurity from the process of Carvedilol (C184625).

Impurity Atenolol Impurity 3; Atenolol Impurity 1
Applications Atenolol Impurity 3. Atenolol Impurity 1.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

Applications A new Sildenafil (S435000) analogue.
References Balayssac, S., et al.: J. Pharm. Biomed. Anal., 50, 602 (2009),

Applications A labelled metabolite of Carvedilol (C184625). It is used in the treatment of hypertension.
References Sponer, G., et al.: J. Cardiovasc. Pharmacol., 9, 317 (1987), Fujimaki, M., ET AL.: Xenobiotica, 20, 1025 (1990), Ruffolo, R., et al.: Eur. J. Clin. Pharmacol., 38, S82 (1990), Schaefer, W.H., et al.: Drug Metab. Dispos., 26, 10, 958 (1998),

Stability Hygroscopic
Applications The optically active isomer of Carvedilol (C184625), a nonselective ß-adrenergic blocker with a1-blocking activity. An antihypertensive used in the treatment of congestive heart failure.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Hirohashi, M., et al.: Arzneim.-Forsch., 40, 735 (1990),

Applications Mixed β-adrenergic blocker and serotonin 5HT1A-receptor antagonist. Antihypertensive; antianginal; antiarrhythmic; antiglaucoma.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Dreshfield, L.J., et al.: Neurochem. Res., 21, 557 (1996), Perez, V., et al.: Lancet, 349, 1594 (1997),

Impurity Rosuvastatin EP Impurity F
Applications (4R,6S)-6-[(1E)-2-[4-(4-Fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]ethenyl]-2,2-dimethyl-1,3-dioxane-4-acetic Acid 1,1-Dimethylethyl Ester (Rosuvastatin EP Impurity F) is a Rosuvastatin (R700500) intermediate as HMG-CoA reductase inhibitor.
References Beck, et al.: J. Med. Chem., 33, 52 (1999),

Applications Bopindolol is an ester prodrug of Pindolol (P468000). Bopindolol is a long acting β-adrenoceptor blocking agent. Bopindolol displays antispasmogenic activity mediated by α1-adrenoceptors and 5-HT2 receptors.
References Turner, D.R. et al.: Br. J. Clin. Pharmacol., 17, 295 (1984); Brodde, O.E. et al.: J. Cardio. Pharmacol., 8, S70 91986); Doggrell, S.A.: Med, Sci. Res., 17, 681 (1989);

Applications Atorvastatin (A791750) impurity.
References Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993); Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996);

Applications Aprindine is a long-acting antiarrhythmic agent, effective when administered orally or intravenously in the treatment of ventricular arrhythmias of varying etiologies.
References Danilo, P. Jr., et al.: Am. Heart. J., 97, 119 (1979); Atarashi, H., et al.: Circulation. J., 66, 553 (2002);

Applications 5-Oxorosuvastatin methyl ester is an intermediate in the synthesis of Rosuvasatatin (calcium salt: R700500), a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor that decreases high-sensitivity C-reactive protein (hsCRP) and cholesterol concentrations in the blood.
References McTaggart, F., et al.: Am. J. Cardiol., 87, 28 (2001); Ridker, P., et al.: Lancet, 373, 1175 (2009)

Impurity Metoprolol EP Impurity O
Applications 1,1’-[(1-Methylethyl)imino]bis[3-[4-(2-methoxyethyl)phenoxy]-2-propanol (Metoprolol EP Impurity O) is an impurity of Metoprolol.
References Gyllenhaal, O., et al.: J. Biochem. Biophys. Methods, 43, 135 (2000), Chester, T., et al.: Anal. Chem., 74, 2801 (2002),

Impurity Atenolol Desmethyl Impurity
Applications Cis-Desmethyl Atenolol is an impurity of Atenolol (A790075), a cardioselective β-adrenergic blocker and antihypertensive agent. Atenolol Desmethyl Impurity
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984);

Applications Labelled Nadolol (N201052). β-Adrenergic blocker. Antihypertensive; antianginal.
References Dreyfuss, J., et al.: J. Clin. Pharmacol., 17, 300 (1977), Sibley, P.L., et al.: Toxicol. Appl. Pharmacol., 44, 379 (1978), Slusarek, L., et al.: Anal. Profiles Drug Subs., 9, 455 (1980),

Impurity Olmesartan Medoxomil EP Impurity D
Applications Olmesartan medoxomil intermediate.
References Birkenhager, W., et al.: J. Hypertens, 17, 873 (1999), Whittaker, A., et al.: Br. J. Cardiol., 12, 125 (2005),

Applications 3-Ethyl 3,5-Didemethyl Memantine is an impurity of Memantine (HCl salt, M218000) which is used as an antiparkinsonian and antispasmodic.
References Rohde, H., et al.: Fortschr. Med., 100, 2023 (1982), Kornhuber, J., et al.: Eur. J. Pharmacol., 166, 589 (1989), Gortelmeyer, R. and Erbler, H.: Arzneimittel-Forsch., 42, 904 (1992)

Impurity Atenolol EP Impurity D
Applications 4-(3-Chloro-2-hydroxypropoxy)benzeneacetamide is an impurity of Atenolol (A790075), a cardioselective β-adrenergic blocker. Atenolol EP Impurity D
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984); Pai, N.R., et al.: J. Chem. Pharma. Rsch., 4, 375 (2012);

Impurity Acebutolol EP Impurity A
Applications 3’-Acetyl-4’-(2,3-epoxypropoxy)butyranilide (Acebutolol EP Impurity A) is a useful intermediate in the preparation of Acebutolol.
References Andresen, B., et al.: Drug Metab. Disposition, 7, 360 (1979),

Applications Protected Atorvastatin.

Applications AICAR is a nucleoside analogue that is able to enter nucleoside pools and is able to significantly increase levels of adenosine during periods of ATP breakdown. Adenosine-regulating agents (ARAs) have been recognized for therapeutic potential in myocardial ischemia. Cardioprotective.
References Mullane, K., et al.: Trends Cardiovasc Med., 3, 227 (1993), Browne, G.J., et al.: J. Biol. Chem., 279, 13, 12220 (2004)

Impurity Timolol EP Impurity G; Timolol BP Impurity G
Stability Moisture Sensitive
Applications 4-​(4-Morpholinyl)​-1,​2,​5-​thiadiazol-​3(2H)​-​one 1-Oxide (Timolol EP Impurity G; Timolol BP Impurity G) is an impurity of Timolol (T4437005), an antihypertensive, an adrenergic blocking agent (1); antiarrhythmic (class II); antianginal; antiglaucoma (2) and antihypertensive (3) agent.
References 1. Wasson, B. et al.: J. Med. Chem. 1972 Jun;15(6):651-5.2. Heel, R. et al.: Drugs. 1979 Jan;17(1):38-55.3. Rofman, et al.: Hypertension. 1980 Sep-Oct;2(5):643-8.

Stability Hygroscopic
Applications A labelled metabolite of Propranolol.
References Walle, T., et al.: Drug Metab. Dispos., 13, 204 (1985), Mason, R., et al.: J. Med. Chem., 34, 869 (1991), Anderson, R., et al.: Biochem. Pharmacol., 52, 341 (1996), Hung, D., et al.: J. Pharmacol. Exp. Ther., 297, 780 (2001),

Applications Labelled Celiprolol. Cardioselective β1-adrenergic blocker. Antihypertensive, antianginal.
References Mazzo, D.J., et al.: Anal. Profiles Drug Subs., 20, 237 (1991), Meininger, C., et al.: Biochem. J., 349, 353 (2000), Ruan, H., et al.: Diabetes, 51, 1319 (2002), Liao, Y., et al.: Circulation, 110, 692 (2004),

Impurity Atenolol USP Related Compound D; Atenolol EP Impurity F
Applications 4,4'-[[(1-methylethyl)imino]bis[(2-hydroxy-3,1-propanediyl)oxy]]bis-benzeneacetamide (Atenolol USP Related Compound D; Atenolol EP Impurity F) is an impurity of Atenolol (A790075), a cardioselective β-adrenergic blocker.
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984); Caplar, V., et al.: Acta. Pharma. Jugoslavica., 33, 71 (1983);

Applications Labelled Dopamine. Endogenous catecholamine with α and β-adrenergic activity. Cardiotonic; antihypotensive.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Carter, J.E., et al.: Anal. Profiles Drug Subs., 11, 257 (1982), Dasta, J.F., et al.: Pharmacotherapy, 6, 304 (1986),

Applications An optically active metabolite of Carvedilol (C184625), a nonselective ß-adrenergic blocker with α1-blocking activity.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package
References Sponer, G., et al.: J. Cardiovasc. Pharmacol., 9, 317 (1987), Fujimaki, M., ET AL.: Xenobiotica, 20, 1025 (1990), Ruffolo, R., et al.: Eur. J. Clin. Pharmacol., 38, S82 (1990), Schaefer, W.H., et al.: Drug Metab. Dispos., 26, 10, 958 (1998),

Rac-Diacetolol is a racemic mixture of two isomers, (+) and (-), of acebutolol. Rac-Diacetolol is used to treat bowel disease, chronic oral inflammation and cardiac arrhythmias. It is also used as an experimental solubility probe in the study of the interactions between drugs and biological membranes. Rac-Diacetolol has been shown to have a low affinity for cytochrome P450 enzymes, which are responsible for metabolizing many drugs in the body. Rac-Diacetolol has been found to reduce plasma concentrations of PCSK9 antibody in patients with inflammatory bowel disease. The drug also has anti-inflammatory properties that may be due to its inhibition of prostaglandin synthesis.

Applications 3-Hydroxy-4-(1-naphthyloxy)-butanenitrile is an intermediate in the synthesis of Nadoxolol (N201040), which is a beta-adrenergic receptor blocker.
References Kappor, M., et al.: Bioorg. Chem., 31, 259 (2003)

Applications A metabolite of the antihypertensive agent, Labetalol (L096500).
References Gal, J., et al.: Res. Comm. Chem. Pathol. Pharmacol., 62, 3 (1988),

Applications Bivalirudin 1-11 Fragment is an impurity of Bivalirudin, a direct thrombin inhibitor acting as an anticoagulant through inhibition of the enzyme thrombin.
References Bertrand, O. et al.: Am. J. Cardio., 110, 599 (2012); Patti, G. et al.: Am. J. Cardio., 110, 478 (2012)

Applications 1-Chloro-3-(1H-indol-4-yloxy)-2-propanol, is an impurity of Pindolol (P468000), a mixed β-adrenergic blocker and serotonin 5HT1A-receptor antagonist. Antihypertensive; antianginal; antiarrhythmic; antiglaucoma.
References Dreshfield, L.J., et al.: Neurochem. Res., 21, 557 (1996), Perez, V., et al.: Lancet, 349, 1594 (1997),

Applications Antihypertensive; antiarrhythmic (class II); antianginal; antiglaucoma agent.
References Wasson, et al.: J. Med. Chem., 15, 651 (1972), Franciosa, et al.: Clin. Pharmacol. Ther., 13, 138 (1972), Heel, R.C., et al.: Drugs, 17, 38 (1979), Rofman, B.A., et al.: Hypertension, 2, 643 (1980), Mazzo, D.J., et al.: Anal. Profiles Drug Subs., 16, 641 (1987),

Applications Labelled Penbutolol (P220500). A β-adrenoceptor antagonist. Antihypertensive.
References Armstrong, D., et al.: Anal. Chem., 66, 1473 (1994), Kato, M., et al.: J. Pharm. Biomed. Anal., 30, 1845 (2003),

Applications An impurity in Simvastatin (S485000).
References Sankar, D. et al.: Asian J. Chem., 21, 4294 (2009); Vuletic, M. et al.: J. Pharmac. Biomed. Anal., 37, 715 (2005);

Applications CMPD101 is a potent and selective GRK2/3 inhibitor.
References Lowe, J.D., et al.: Mol. Pharmacol., 88, 347 (2015); Ikeda, S., et al.: PCT Int. Appl. WO 2007034846 A1 20070329. Mar 29, 2007

Applications 4-Methyl-1-hydrazinophthalazine is used in the synthesis of novel phthalazine derivatives as antihypertensive agents.

Applications A metabolite of Eplerenone. Used in combination therapy for treatment of cardiovascular disorders.
References Staessen, J., et al.: J. Endocrinol., 91, 457 (1981), de Gasparo, M., et al.: J. Pharmacol. Exp. Ther., 240, 650 (1987), MacFadyen, R., et al.: Cardiovasc. Res., 35, 30 (1997),

Impurity Atorvastatin 2-Hydroxy Lactone
Stability Hygroscopic
Applications A metabolite of Atorvastatin, a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is the only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia.