Bêta-bloquants

<p>Applications Nonpeptide endothelin ETA receptor antagonist. Antihypertensive.<br>References Riechers, H., et al.: J. Med. Chem., 39, 2123 (1996), Billman, G.E., et al.: Curr. Opin. Invest. Drugs, 3, 1483 (2002), Vatter, H., et al.: Clin. Neuropharmacol., 26, 73 (2003),<br></p>

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

<p>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.<br>References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984); Robbiano, L., et.al., Cancer Res., 51, 2273-2279, (1991);<br></p>

<p>Applications A metabolite of Spironolactone.<br>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),<br></p>

<p>Applications Antihypertensive; antiarrhythmic (class II); antianginal; antiglaucoma agent.<br>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),<br></p>

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

<p>Impurity Carvedilol EP Impurity D; Carvedilol USP-D<br>Applications 4-(2,3-Epoxypropoxy)carbazole (Carvedilol EP Impurity D; Carvedilol USP-D) is an intermediate in the synthesis of Carvedilol (C184625).<br></p>

<p>Impurity Timolol EP Impurity F; Timolol BP Impurity F; Timolol USP Related Compound F<br>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.<br>References Wasson, B., et al.: J. Med. Chem., 15, 651 (1972), Tokunaga, M., et al.: Sci., 277, 936 (1997),<br></p>

<p>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.<br>References McTaggart, F., et al.: Am. J. Cardiol., 87, 28 (2001); Ridker, P., et al.: Lancet, 373, 1175 (2009)<br></p>

<p>Impurity Metoprolol EP Impurity B<br>Applications 4-(2-Methoxyethyl)phenol (Metoprolol EP Impurity B) is an impurity of Metoprolol.<br>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)<br></p>

<p>Applications A β-adrenoceptor antagonist. Antihypertensive.<br>References Armstrong, D., et al.: Anal. Chem., 66, 1473 (1994), Kato, M., et al.: J. Pharm. Biomed. Anal., 30, 1845 (2003),<br></p>

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

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

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

<p>Impurity Carvedilol Impurity A; Carvedilol USP A<br>Applications An impurity from the process of Carvedilol (C184625). Carvedilol impurity A. Carvedilol USP A.<br></p>

<p>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.<br>References Hoffman, W.F., et al.: J. Med. Chem., 29, 849 (1986), Mol, M.J., et al.: Lancet, 2, 936 (1986)<br></p>

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

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

<p>Impurity Timolol EP Impurity A; Timolol BP Impurity A; Timolol USP Related Compound A<br>Applications (R)-Timolol (Timolol EP Impurity A; Timolol BP Impurity A; Timolol USP Related Compound A) is an antihypertensive agent that increases ocular blood flow and reduces intraocular pressure. (R)-Timolol is an β-adrenergic blocking agent that binds only to nonspecific sites in the particulate fraction of the heart, lungs, and brain.<br>References Rotmensch, H. et al.: J. Clinical. Pharmacol., 33, 544 (1993); Chiou, G. &amp; Chen. Y., J. Ocular. Pharmacol., 8, 183 (1992); Chiou, G. et al.: J. Ocular. Pharmacol., 6, 23 (1990); Tocco, D. et al.: Drug Met. Disposit., 4, 323 (1976)<br></p>

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

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

<p>Impurity Rosuvastatin EP Impurity F<br>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.<br>References Beck, et al.: J. Med. Chem., 33, 52 (1999),<br></p>

<p>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.<br>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);<br></p>

<p>Impurity Rosuvastatin EP Impurity G<br>Stability Hygroscopic<br>Applications ent-Rosuvastatin is an enantiomer of Rosuvastatin (R700500), an impurity which acts as a selective, competitive HMG-CoA reductase inhibitor (1). Antilipemic (2,3).<br>References 1. Watanabe, M. et al.: Bioorg. Med. Chem. 1997 Feb;5(2):437-44.2. Lee, E. et al.: Clin. Pharmacol. Ther. 2005 Oct;78(4):330-41.3. Ferdinand, C. et al.: Am. J. Cardiol. 2006 Jan 15;97(2):229-35.<br></p>

<p>Impurity Verapamil EP Impurity J HCl<br>Applications Nor Verapamil Hydrochloride (Verapamil EP Impurity J HCl) is a metabolite of Verapamil.<br>References Mutlib, A.E., et al.: The Journal of Pharm. &amp; Exp. Therapeutics, 252, 2, 593 (1989)<br></p>

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

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

<p>Applications Labelled Nadolol (N201052). β-Adrenergic blocker. Antihypertensive; antianginal.<br>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),<br></p>

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

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

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

<p>Applications Protected Atorvastatin.<br></p>

<p>Applications Pindolol (P468000) impurity.<br></p>

<p>Impurity Atorvastatin Pyrrolidone Analog (USP)<br>Stability Light Sensitive<br>Applications A photodegradation product of Atorvastatin (a cyclic impurity of Atorvastatin). Atorvastatin Pyrrolidone Analog (USP).<br>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),<br></p>

<p>Impurity Timolol EP Impurity G; Timolol BP Impurity G<br>Stability Moisture Sensitive<br>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.<br>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.<br></p>

<p>Impurity Ezetimibe Tetrahydropyran Impurity<br>Applications Ezetimibe (E975000) tetrahydropyran impurity.<br></p>

<p>Stability Hygroscopic<br>Applications A labelled metabolite of Propranolol.<br>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),<br></p>

<p>Applications Labelled Celiprolol. Cardioselective β1-adrenergic blocker. Antihypertensive, antianginal.<br>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),<br></p>

<p>Impurity Atenolol USP Related Compound D; Atenolol EP Impurity F<br>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.<br>References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984); Caplar, V., et al.: Acta. Pharma. Jugoslavica., 33, 71 (1983);<br></p>

<p>Stability Hygroscopic<br>Applications Pravastatin Lactone is a metabolite of Pravastatin (P702000).<br>References Boberg, M., et al.: Drug Metab. Dispos., 25, 321 (1997), Neuvonen, P., et al.: Clin. Pharmacol. Ther., 63, 332 (1998), Boyd, R., et al.: J. Clin. Pharmacol., 40, 91 (2000),<br></p>