Bêta-bloquants

<p>Stability Hygroscopic<br>Applications Labelled Mexiletine (M340800). Antiarrhythmic (class IB).<br>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),<br></p>

<p>Applications 1,1'-[(1-Methylethyl)imino]bis[3-(1-naphthalenyloxy)-2-propanol is an impurity of Propranolol (P831800), an β−Adrenergic blocker used as a antihypertensive and antilanginal agent.<br>References Helboe, P., et al.: J. Chromatography., 245, 229 (1982); Helboe, P., et al.: J. Chromatography., 245, 229 (1982);<br></p>

<p>Impurity Metoprolol EP Impurity A<br>Applications C-Desmethyl Metoprolol (Metoprolol EP Impurity A) is a new byproduct detected in Metoprolol tartrate. Metoprolol impurity.<br>References Erickson, M., et al.: J. Pharma. Biomed. Analysis, 13, 567 (1995), Phinney, K., et al.: Chirality, 15, 287 (2003), Zheng, J., et al.: Anal. Chem., 78, 1535 (2006),<br></p>

<p>Impurity Timolol EP Impurity H<br>Applications 2-(3-(tert-Butylamino)-2-hydroxypropyl)-4-morpholino-1,2,5-thiadiazol-3(2H)-one is a impurity of Timolol (T443710), an antihypertensive; antiarrhythmic (class II); antianginal; antiglaucoma agent.<br>References Lacroix, P.M., et. al.: Chirality, 6, 484 (1994); 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>Applications An antiarrhythmic agent isolated from Rauwolfia serpentina.<br>References Galarreta, B., et al.: Bioorg. Med. Chem., 16, 6689 (2008), Sun, L., et al.: Plant Mol. Biol., 67, 455 (2008), Ruiz-May, E., et al.: Mol. Biotechnol., 41, 278 (2009),<br></p>

<p>Impurity Metoprolol EP Impurity N<br>Applications 3-Isopropylamino-1,2-propanediol (Metoprolol EP Impurity N) is a versatile organic building block, used in different chemical synthesis. It is used in the preparation of heterocyclic propanolamines, which are shown to have β-adrenergic antagonist activity.<br>References Dean, V. et al.: Drug Design and Discovery,10, 89 (1993);<br></p>

<p>Applications A compound present in olive oil. An important fine chemical intermediate with broad prospects for application development.<br>References Shu, Y., et al.: Guangdong Huagong, 37, 108 (2010), Papadopoulos, G., et al.: J Am Oil Chem Soc, 68, 669 (1991),<br></p>

<p>Applications Pindolol (P468000) impurity.<br>References Ohia, S., et al.: Pharmacol. Exp. Ther., 255, 11 (1990), Juteau, H., et al.: Bioorg. Med. Chem., 9, 1977 (2001),<br></p>

<p>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.<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>Applications An isomer of the antiarrhythmic, antiglaucoma agent Timolol (T443700).<br>References Marini, R.D. et al.: Anal. Chim. Acta, 531, 131 (2005);<br></p>

<p>Applications 2-(2-Aminoethoxy)anisole is used as an additive to vinylphosphonic acid esters and acrylonitrile forming compounds displaying hypotensive activity. An impurity from the process of Carvedilol (C184625)<br>References Reznik, V. et al.: Russ. Chem. Bull., 48, 979, (1999); Hirohashi, M., et al.: Arzneim.-Forsch., 40, 735 (1990), Packer, M., et al.: N. Engl. J. Med., 334, 1349 (1996),<br></p>

<p>Impurity Clonidine EP Impurity A<br>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.<br>References Czeskis, B., et al.: J. Labelled Comp. Radiopharm., 47, 699 (2004)<br></p>

<p>Applications 2-[3-(Aminosulfonyl)-4-chlorobenzoyl]-benzonic Acid is a potential metabolite of Chlorthalidone.<br>References Salado C., et al.: J. Chromatography. Biomed. App., 690, 195 (1997);<br></p>

<p>Applications A metabolite of Carvedilol (C184625). It is used in the treatment of hypertension.<br>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),<br></p>

<p>Applications Isometheptene Maleate belongs to a group of sympathomimetic amine and shows very little antihypertensive activity. Isometheptene Maleate is used as an antispasmodic drug.<br>References Vidrio, H. et al.: J. Pharmacol. Exp. Therap., 187, 308 (1973); Taylor, W.G. et al.: Drug Metab. Disp., 5, 564 (1977);<br></p>

<p>Applications 2-Oxo-Zoniporide is an metabolite of Zoniporide, a potent and selective inhibitor of human sodium-hydrogen exchanger isoform1(NHE-1) and protects against cardiac ischemia-reperfusion injury.<br>References Ross, T.W., et al.: Cardiovascular. Drug. Reviews., 21, 17 (2003); Deepak, D., et al.: Drug. Metabol. Dispos., 38, 641 (2010);<br></p>

<p>Applications A labelled 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 Diazoxide-d3 is the labeled analogue of Diazoxide (D417305), which reduces status epilepticus neuron damage in diabetes.<br>References Baba, A., et al.: J. Neurosci., 23, 7737 (2003); Bancila, V., et al.: J. Neurochem., 90, 1243 (2004); Bancila, V., et al.: J. Biol. Chem., 280, 8793 (2005)<br></p>

<p>Impurity Fluocinolone Acetonide EP Impurity E<br>Stability Hygroscopic<br>Applications (6α,9β,11β,16α)-9,11-Epoxy-6-fluoro-21-hydroxy-16,17-[(1-methylethylidene)bis(oxy)]pregna-1,4-diene-3,20-dione, can be used in the production of fluocinolone acetonide (F455800).<br>References Grinenko, G.S, Khimiko-Farmatsevticheskii Zhurnal, 12, 110 (1978), Sammul, et al.: J. Assoc. Off. Agric. Chem., 47, 952 (1964), Emerson, M.V., et al.: BioDrugs, 21, 245 (2007),<br></p>

<p>Applications An optically active metabolite of Carvedilol (C184625), a nonselective ß-adrenergic blocker with α1-blocking activity.<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 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),<br></p>

<p>Applications A labelled inhibitor of glucose synthesis.<br>References Garcia-Salguero, L. et al.: Arch. Int. Physiol., Biochim. Biophys., 99, 237, (1991); Martirosyan, A., et al.: Biochem. Pharmacol., 68, 1729 (2004);<br></p>

<p>Applications Labelled 7α-Hydroxy-4-cholesten-3-one (H825130). 7α-Hydroxy-4-cholesten-3-one is a metabolite of Cholesterol (C432501).<br>References Connor, W., et al.: J, Clin. Invest., 48, 1363 (1969),<br></p>

<p>Applications Mixed β-adrenergic blocker and serotonin 5HT1A-receptor antagonist. Antihypertensive; antianginal; antiarrhythmic; antiglaucoma.<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 Dreshfield, L.J., et al.: Neurochem. Res., 21, 557 (1996), Perez, V., et al.: Lancet, 349, 1594 (1997),<br></p>

<p>Impurity Atenolol 2-Hydroxy Impurity<br>Applications Hydroxyatenolol is a metabolite of Atenolol (A790075); a cardioselective β-adrenergic blocker, antihypertensive, antianginal, and antiarrhythmic (class II). Atenolol 2-Hydroxy Impurity<br>References Escher, B., et al.: Environ. Sci. Technol., 40, 7402 (2006); Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984)<br></p>

<p>Applications Labelled Amlodipine (A633495). A dihydropyridine calcium channel blocker; activity resides mainly in the (-)-isomer.<br>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),<br></p>

<p>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.<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 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<br></p>

<p>Impurity Timolol EP Impurity D; Timolol BP Impurity D; Timolol USP Related Compound D<br>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.<br>References Bodor, N., et al.: J. Med. Chem., 31, 100 (1988),<br></p>

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

<p>Applications An optically active metabolite of Carvedilol (C184625), a nonselective ß-adrenergic blocker with α1-blocking activity.<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 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),<br></p>

<p>Applications A dextrorotatory stereoizomer of Quinine. Antiarrhythmic (class IA). Antimalarial.<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 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),<br></p>

<p>Impurity Atenolol EP Impurity E<br>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<br>References Caplar, V., et al.: Anal. Profiles Drug Subs., 13, 1 (1984);<br></p>

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

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

<p>Applications Antihypertensive; diuretic.<br>References Piala, J.J., et al.: J. Pharmacol. Exp. Ther., 134, 273 (1961), Orzech, C.E., et al.: Anal. Profiles Drug Subs., 7, 297 (1978),<br></p>

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

<p>Applications Carvedilol is a nonselective β-adrenergic blocker with α1-blocking activity. Carvedilol is an antihypertensive used in the treatment of congestive heart failure.<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 Hirohashi, M., et al.: Arzneim.-Forsch., 40, 735 (1990); Packer, M., et al.: N. Engl. J. Med., 334, 1349 (1996);<br></p>

<p>Applications Diltiazem (D460620) intermediate (impurity B).<br>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),<br></p>

<p>Applications Carvedilol (C184625) derivative.<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>Stability Hygroscopic<br>Applications Rosuvastatin tert-Butyl Ester, is a metabolite of Rosuvastatin (R700500) a selective, competitive HMG-CoA reductase inhibitor.<br>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),<br></p>

<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>