Bêta-bloquants

Applications Befunolol is a β-adrenergic blocker with an intrinsic sympathomimetic action. But it can work as a β-adrenergic partial agonist in isolated organs.
References Nakano, J., et al.: Chem. Pharm. Bull., 36, 1399 (1988); Takayanagi, I., et al.: Gen. Pharmacol., 20, 417 (1989); Koike, K., et al.: Gen. Pharmacol., 25, 1477 (1994)

Applications (2R,3S)-rel-Nadolol-N-[(2R,3S)-rel-Nadolol-de(N-tert-butyl)]is an impurity of Nadolol (N201050), a 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)

Applications Labelled Amlodipine (A633495). A dihydropyridine calcium channel blocker; activity resides mainly in the (-)-isomer.
References Arrowsmith, J.E., et al.: J. Med. Chem., 29, 1696 (1986), Burges, R.A., et al.: J. Cardiovasc. Pharmacol., 9, 110 (1987), Haria, M., et al.: Drugs, 50, 560 (1995),

Applications Asperosaponin VI is a steroidal extract with anti-inflammatory and antinociceptive activity. long term use has been seen to attenuate cardiac dysfunction.
References Choi, J. et al.: J. Med. Food, 8, 78 (2005); Li, C. et al.: Food. Chem. Toxicol., 8, 1432 (2012);

Applications 6-Oxo Simvastatin is an analog of Simvastatin (S485000), a HMG-CoA reductase inhibitor.
References Joshua, H., et al.: J. Antibiot., 44, 366 (1991),

Impurity Hydrochlorothiazide EP Impurity C
Applications N-[[7-(Aminosulfonyl)-6-chloro-2,3-dihydro-1,1-dioxo-4H-1,2,4-benzothiadiazin-4-yl]methyl]-6-chloro-3,4-dihydro-1,1-dioxo-2H-1,2,4-benzothiadiazine-7-sulfonamide (Hydrochlorothiazide EP Impurity C) is an impurity in bulk Hydrochlorothiazide. Dimer Impurity C.
References Daniels, S.L., et al.: J. Pharm. Sci., 70, 211 (1981), Fang, X., et al.: Pharm. Res., 14, 691 (1997),

Applications 2-Phenylphenol is an agricultural fungicide and is no longer used as a food additive (1). It has been associated with the incidence of bladder cancer in male rats which may be related to its primary metabolite, phenylhydroquinone (2). Drinking water contaminant candidate list 3 (CCL 3) compound as per United States Environmental Protection Agency (EPA). Environmental contaminants; Food contaminants.
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 1. Gouin T. et al.: Environ Pollut. 2012 Jun;165:208-14. 2. Balakrishnan, S. et al.: Environ Mol Mutagen. 2016 Apr;57(3):210-9

Applications N6-Isopentenyladenosine has antiproliferative activity on MCF-7 breast cancer cells.
References Rajabi, M. et al.; DNA Cell Biol.; 29, 687 (2010)

Impurity Timolol EP Impurity D; Timolol BP Impurity D; Timolol USP Related Compound D
Applications 3-Hydroxy-4-morpholino-1,2,5-thiazole (Timolol EP Impurity D; Timolol BP Impurity D; Timolol USP Related Compound D) is an intermediate for the preparation of Timolol.
References Bodor, N., et al.: J. Med. Chem., 31, 100 (1988),

Applications α-Propyl-α-(1-demethylethyl)-Verapamil is an impurity of Verapamil (V125000, HCl salt) which is a calcium channel blocker.
References Atlas, D, and Adler, M.: Proc. Natl. Acad. Sci. USA, 78, 1237 (1981), Janis, R., et al.: Adv. Drug. Res., 16, 309 (1987)

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),

Applications A dextrorotatory stereoizomer of Quinine. Antiarrhythmic (class IA). Antimalarial.
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 Loutfy, M.A., et al.: Anal. Profiles Drug Subs., 12, 483 (1983), Mason, J. W., et al.: Ann. N. Y. Acad. Sci., 432, 162 (1984),

Impurity Atenolol EP Impurity E
Applications 4,4'-[(2-Hydroxy-1,3-propanediyl)bis(oxy)]bis-benzeneacetamide is an impurity of Atenolol (A790075), a cardioselective β-adrenergic blocker. Atenolol EP Impurity E
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984);

Applications Labelled Diltiazem (D460620). A calcium channel blocher with vasodilating activity. Antianginal; antihypertensive; antiarrhythmic (class IV).
References Sato, et al.: Arzneim.-Forsch., 21, 1338 (1971), Smirnov, S.R.: Eur. J. Pharmacol., 360, 81 (1998), Hansson, L., et al.: Lancet, 356, 359 (2000),

Applications Labelled Ouabain (O714500). A cardiac glycoside that inhibits Na(+)/K(+) ATPase. It regulates transcription of MDR (increase, Pgp) and MRP (increase MRP1 and decrease CFTR, cyctic fibrosis transport receptor or cAMP-activated Cl- channel) genes, also alters localization of MRP1.
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 Padilha, A.S. et al.: Clin. Exp. Pharmacol. Physiol., 35, 801 (2008); Blaustein, M.P. et al.: Clin. Exp. Hypertens. 20, 691 (1998); van Huysse, J.W. et al.: Clin. Exp. Hypertens. 20, 657 (1998);

Applications Propoxyphenyl-thiohydroxyhomosildenafil is an analogue of Hydroxythiohomo Sildenafil (H963150).
References Balayssac, S., et. al.: J. Pharmaceut. Biomed., 63, 135 (2012)

Applications 4’-Hydroxyphenprocoumon is a metabolite of the oral anticoagulant Phenprocoumon (P318820).
References De Vries, J. et al.: J. Chrom. Biomed. Appl., 529, 479 (1990);

Applications Rosuvastatin Methyl Ester is an impurity of Rosuvastatin (R700500) in the pharmaceutical dosage forms under forced degradation conditions.
References Lennernas, H., et al.: Clin. Pharmacokinet., 32, 403 (1997), Kivisto, K., et al.: Br. J. Clin. Pharmacol., 46, 49 (1998), Lan, K., et al.: J. Pharm. Biomed. Anal., 44, 540 (2007),

Impurity Tranexamic EP Impurity A
Applications Tranexamic Acid Dimer (Tranexamic EP Impurity A) is a Tranexamic Acid (T714505) impurity.

Applications N-Nitrosometoprolol is an N-nitroso derivative of rac Metoprolol(M338815), which is a β1 selective aryloxypropanolamine andrenergic antagonist. Used in the treatment of a variety of cardiovascular disorder. N-Nitrosometoprolol can be used to assess human and rat hepatocytes.
References McGourty, J.C., et al.: Br. J. Clin. Pharmacol. 20, 555 (1985); Lennard, M.S., et al.: Biochem. Pharmacol., 35, 2757 (1986); Martelli, A., In Vivo, 11, 189-194, (1997);

Applications Carvedilol is a nonselective β-adrenergic blocker with α1-blocking activity. Carvedilol is 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); Packer, M., et al.: N. Engl. J. Med., 334, 1349 (1996);

Applications An enantiomeric impurity of Ezetimibe (E975005), an antihyperlipoproteinemic and cholesterol absorption inhibitor.

Applications Diltiazem (D460620) intermediate (impurity B).
References Chaffman, M., et al.: Drugs, 29, 387 (1985), Kamath, B., et al.: J. Pharm. Biomed. Anal., 11, 407 (1993), Chankvetadze, B., et al.: J. Pharm. Biomed. Anal., 27, 161 (2002),

Applications Carvedilol (C184625) derivative.
Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

Stability Hygroscopic
Applications Rosuvastatin tert-Butyl Ester, is a metabolite of Rosuvastatin (R700500) a selective, competitive HMG-CoA reductase inhibitor.
References Watanabe, M., et al.: Bioorg. Med. Chem., 5, 437 (1997), Lee, E., et al.: Clin. Pharmacol. Ther., 78, 330 (2005), Ferdinand, K.C., et al.: Am. J. Cardiol., 97, 229 (2006),

Stability Hygroscopic
Applications (S)-Penbutolol Sulfate is an isomer of Penbutolol (P220500), a β-adrenoceptor antagonist. Antihypertensive.
References Lassen, J.B.: Eur. J. Pharmacol., 47, 351 (1978), Lund, J., et al.: Acta Pharmacol. Toxicol., 51, 351, (1982),

Applications N-Nitrosoatenolol is an N-nitroso derivative of Atenolol (A790075), which is a cardioselective β-adrenergic blocker. Antihypertensive, antianginal, antiarrhythmic (class II). N-Nitrosoatenolol can be used for its genotoxic effect in rat and human hepatocytes.
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984); Robbiano, L., et.al., Cancer Res., 51, 2273-2279, (1991);

Applications A metabolite of Spironolactone.
References Gochman, N., et al.: J. Pharmacol. Exp. Ther., 135, 312 (1962), Tori, K., et al.: Steroids, 4, 713 (1964), Solymoss, B., et al.: Toxicol. Appli. Pharmacol., 18, 586 (1971),

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),

Impurity Atenolol EP Impurity C
Applications 4-(2,3-Epoxypropoxy)phenylacetamide (Atenolol EP Impurity C) is an impurity of Atenolol, a cardioselective β-adrenergic blocker.
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984)

Stability Hygroscopic
Applications Labelled Mexiletine (M340800). Antiarrhythmic (class IB).
References Singh, E.M., et al.: Br. J. Pharmacol., 44, 1 (1972), Scott, K.N., et al.: Drug Metab. Dispos., 1, 506 (1973), Chew, C.Y.C., et al.: Drugs, 17, 161 (1979), Abounassif, M.A., et al.: Anal. Profiles Drug Subs., 20, 433 (1991),

Impurity Clonidine EP Impurity A
Applications 1-Acetyl-2-imidazolidinone (Clonidine EP Impurity A) is a synthetic reagent used in the preparation of triple [14C]-labelled moxonidine which is an antihypertensive compound.
References Czeskis, B., et al.: J. Labelled Comp. Radiopharm., 47, 699 (2004)

Impurity Timolol EP Impurity F; Timolol BP Impurity F; Timolol USP Related Compound F
Applications 3-Chloro-4-morpholino-1,2,5-thiadiazole (Timolol EP Impurity F; Timolol BP Impurity F; Timolol USP Related Compound F) is an intermediate for the synthesis of Timolol.
References Wasson, B., et al.: J. Med. Chem., 15, 651 (1972), Tokunaga, M., et al.: Sci., 277, 936 (1997),

Applications Labelled Torsemide (T548750). Used as a diuretic.
References Lesne, M., et al.: In. J. Clin. Pharmacol. Ther. Toxicol., 20, 382 (1982), Brater, D.C., et al.: Clin. Pharmacol. Ther., 42, 187 (1987),

Impurity Metoprolol EP Impurity B
Applications 4-(2-Methoxyethyl)phenol (Metoprolol EP Impurity B) is an impurity of Metoprolol.
References McGourty, J., et al.: Br. J. Clin. Pharmacol., 20, 555 (1985), Zhou, H., et al.: Clin. Pharmacol. Ther., 47, 686 (1990), Koyama, E., et al.: J. Pharmacol. Exp. Ther., 271, 860 (1994)

Applications 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 Labelled (S)-Atenolol (A790080). Cardioselective β-adrenergic blocker. Antihypertensive, antianginal, antiarrhythmic (class II).
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984),

Applications Cardioselective β-adrenergic blocker. Antihypertensive, antianginal, antiarrhythmic (class II).
References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984),

Impurity Carvedilol EP Impurity E; Carvedilol Impurity E; Carvedilol USP E
Applications 2-(2-Methoxyphenoxy)ethylamine Hydrochloride (Carvedilol EP Impurity E; Carvedilol Impurity E; Carvedilol USP E) is an impurity of Carvedilol synthesis.
References Smith, L., et al.: J. Med. Chem., 20, 1653 (1977),

Applications 2-Fluoroadenosine is a fluorinated analog of Adenoside (A280400) nucleotide.
References Long, X., et al.: J. Pharmacol. Exper. Ther., 335, 781 (2010); Ham, M., et al.: J. Pharmacol. Exper. Ther., 335, 607 (2010);

Applications Tenivastatin Calcium is derived from Simvastatin (S485000), which is a synthetic derivative of a fermentation product of Aspergillus terreus. A competitive inhibitor of HMG-CoA reductase. A synthetic analog of Lovastatin. Antilipemic. Simvastatin, the drug, is sold under the trade name Zocor.
References Hoffman, W.F., et al.: J. Med. Chem., 29, 849 (1986), Mol, M.J., et al.: Lancet, 2, 936 (1986)