Beta Blockers

Applications Nebivolol Hydrochloride is a highly selective β1-adrenoceptor antagonist. References Van de Water, A., et al.: J. Cardiovasc. Pharmacol., 11, 552 (1988), De Cree, J., et al.: Angiology, 41, 95 (1990);

Amino-alcohols, other than those containing more than one kind of oxygen function, their ethers and esters, salts thereof, nesoi

Impurity Bisoprolol Carboxylic Acid Impurity Applications The major metabolite of Bisoprolol (B510500). References Heberer, T., et al.: Toxicol. Lett., 131, 5 (2002), Boxall, A., et al.: Environ. Sci. Technol., 38, 368A (2004), Huschek, G., et al.: Environ. Toxicol., 19, 226 (2004), Larsen, T., et al.: J. Biotechnol., 113, 295 (2004)

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);

Impurity Atorvastatin Pyrrolidone Analog (USP) Stability Light Sensitive Applications A photodegradation product of Atorvastatin (a cyclic impurity of Atorvastatin). Atorvastatin Pyrrolidone Analog (USP). References Roger, D., et al.: Clin. Exp. Dermatol., 19, 88 (1994), Cosa, G., et al.: Photochem. Photobiol., 80, 159 (2004), Kerwin, B., et al.: J. Pharm. Sci., 96, 1468 (2007),

Applications 2-Isobutyryl-N-phenyl-3-phenylacrylamide is the labeled analogue of 2-Isobutyryl-N-phenyl-3-phenylacrylamide (I781040), an intermediate for the synthesis of Atorvastatin-d5 Sodium Salt (A791753), the labeled analogue of Atorvastatin (A791750) (1,2,3). Atorvastatin is the only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia. 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) Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993) (2) Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996) (3) Whitfield, L.R., et al.: Eur. J. Drug Metab. Pharmacokinet., 25, 97 (2000)

Applications Valsartan intermediate. References Criscione, L., et al.: Brit. J. Pharmacol., 110, 761 (1993), Muller, P., et al.: Eur. J. Clin. Pharmacol., 47, 231 (1994)

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);

Ether-phenols, ether-alcohol-phenols and their halogenated, sulfonated, nitrated or nitrosated derivatives

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),

Applications Flecainide is an antiarrhythmic (class IC). References Hodess, A.B., et al.: J. Cardiovasc. Pharmacol., 1, 427 (1979), Somani, P., et al.: Clin. Pharmacol. Ther., 27, 464 (1980), Alessi-Severini, S., et al.: Anal. Profiles Drug Subs. Excip., 21, 169 (1992)

Applications The essential intermediate metabolite from which the active metabolite of Clopidogel is formed. References Feliste, R., et al.: Thromb. Res., 48, 403 (1987), Savi, P., et al.: Biochem. Pharmacol., 44, 527 (1992), Herbert, J., et al.: Cardiovasc Drug. Rev., 11, 180 (1993), Sugidachi, A., et al.: B. J. Pharmacol., 132, 47 (2001)

Applications Labelled Pitavastatin. A HMG CoA reductase inhibitor. An antilipemic. References Yen, H., et al.: J. Clin. Invest., 98, 1253 (1996), Zou, Y., et al.: J. Biol. Chem., 274, 9760 (1999), Sun, X., et al.: Cancer Res., et al.: 61, 3382 (2001), Ladas, E.J., et al.: Clin. Oncol., 22, 517 (2004),

Applications O-Des[2-aminoethyl]-O-carboxymethyl-dehydroamlodipine is the metablolite of Amlodipine (A633495), a long-acting calcium channel blocker that is commonly used as an anti-hypertensive in the treatment of cardiovascular conditions. 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 The labelled R-enantiomer of Propranolol (P831800). β−Adrenergic blocker. Antihypertensive; antianginal; antiarrhythmic (class II). References Bond, et al.: Nature, 213, 721 (1967), Hansteen, V., et al.: Br. Med. J., 284, 155 (1982), Diamond, S., et al.: J. Clin. Pharmacol., 28, 193 (1988),

Stability Moisture Sensitive Applications Oxyfedrine acts as a vasodilator affecting the coronary base flow. References Baraka, Y. et al.: J. Drug Res., 12, 161 (1980);

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 An inactive Amiloride analogue References Besterman, J., et al.: J. Biol. Chem., 264, 2324 (1989), Venanzi, C., et al.: J. Med. Chem., 35, 1643 (1992), Yamamoto, T., et al.: Chem. Pharm. Bull., 45, 1282 (1997),

Applications Bisoprolol-d7 Hemifumarate, is the labeled analogue of Bisoprolol Hemifumarate (B510500), a selective β-adrenergic blocker. Used as an antihypertensive. References Tattersfield, A.E., et al.: Brit. J. Clin. Pharmacol., 18, 343 (1984), Kohli, R.S., et al.: Eur. Heart J., 6, 845 (1985), Zachariah, P.K., et al.: Clin. Ther., 15, 779 (1993),

Applications A labelled metabolite of Pitavastatin. Recent studies have shown that conversion between acid and lactone forms occurs in the body, drug-drug interaction should be considered on both acid and lactone forms. The inhibitory effects of statins on CYP metabolic activities and MDR1 transporting activity were investigated using human liver microsomes and MDR1-overexpressing LLC-GA5-COL150 cells. References Wang, J., et al.: Drug Metab. Dispos., 30, 1352 (2002), Yamada, I., et al.: Xenobiotica, 33, 789 (2003), Fujino, H., et al.: Xenobiotica, 34, 961 (2004), Ando, H., et al.: Br. J. Clin. Pharmacol., 60, 494 (2005),

Applications Used as an antihypertensive and antianginal. References Gross, G.J., et al.: Gen. Pharmacol., 14, 677 (1983), Molyvdas, P.A. and Sperelakis, N.: J. Cardiovasc. Pharmacol., 8, 449 (1986), Mizuno, K., et al.: Res. Comm. Chem. Pathol. Pharmacol., 52, 3 (1986)