Bloqueadores Beta

<p>Stability Hygroscopic<br>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.<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),<br></p>

<p>Applications Inhibits the enzyme HMG-CoA reductase in vitro.<br>References Endo, A., et al.: J. Antibiot., 32, 852 (1979), Alberts, A.W., et al.: Drug Invest., 2 (Suppl. 2), 9 (1990), Kuroda, M., et al.: Biochim. Biophys. Acta, 486, 70 (1977),<br></p>

<p>Applications An enantiomeric impurity of Ezetimibe (E975005), an antihyperlipoproteinemic and cholesterol absorption inhibitor.<br></p>

<p>Impurity Fluocinolone Acetonide EP Impurity B<br>Applications (6α,11β,16α,17α)-6,9-Difluoro-11-hydroxy-16,17-[(1-methylethylidene)bis(oxy)]-3-oxoandrosta-1,4-diene-17-carboxylic Acid, is a derivative of Fluocinolone Acetonide (F455800), which is a Corticosteroid, used in dermatology to reduce skin inflammation and relieve itching.<br>References 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 Epinephrine (E588585) derivative formed in injection solutions and eye drops during sterilization and storage of L-Epinephrine Bitartrate.<br>References De Mol, N.J. et al.: Pharmac. Week., 117, 1 (1982); Liu, C. et al.: Yao. Fen. Zaz., 2, 200 (1982);<br></p>

<p>Applications A carvedilol Impurity.<br></p>

<p>Impurity Rosuvastatin EP Impurity B<br>Stability Hygroscopic<br>Applications A diastereomer of Rosuvastatin (R700500) used for treatment, prevention and combination therapy of lipid-related disorders. Rosuvastatin EP Impurity B<br></p>

<p>Applications Norepinephrine Sulfonic Acid is a derivative of DL-Norepinephrine Hydrochloride (N674500), antagonist of dibutyryl cyclic-AMP in the regulation of narcosis. Norepinephrine modulates human dendritic cell activation by altering cytokine release.<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 Piguet, P., et al.: J. Exp. Med., 173, 673 (1991), Hosoi, J., et al.: Nature, 363, 159 (1993), Elenkov, I., et al.: Pharmacol. Rev., 52, 595 (2000), Kaplan, D., et al.: Immunity, 23, 611 (2005),<br></p>

<p>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.<br>References Mullane, K., et al.: Trends Cardiovasc Med., 3, 227 (1993), Browne, G.J., et al.: J. Biol. Chem., 279, 13, 12220 (2004)<br></p>

<p>Applications A labelled antihypertensive. An angiotensin converting enzyme (ACE) inhibitor, converted to active, diacid metabolite.<br>References Teetz, V., et al.: Arzneim.-Forsch., 34, 1399 (1984), Ruggenenti, P., et al.: Lancet, 352, (1998), Bosch, J., et al.: Br. Med. J., 324, 1 (2002),<br></p>

<p>Applications Nicergoline-d3 is the labeled analogue of Nicergoline(N394550), a drug used for age-dependent cognitive impairment such as Alzheimers disease and other types of dementia.<br>References Caraci, F., et. al.: Brain Res., 1047, 30 (2005); Mizuno, T., et. al.: Brain Res., 1066, 78 (2005)<br></p>

<p>Impurity Ezetimibe Ketone (USP)<br>Applications Phase-I metabolite of Ezetimibe (E975000).<br>References Shah, V., et al: J. Pharm. Sci., 17, 1551 (2000), Van Heek, M., et al.: Br. J. Pharmacol., 134, 409 (2001), Watts, G., et al.: Clin. Sci.,103, 595 (2002), Ghosal, A., et al.: Drug Metab. Dispos., 32, 314 (2004), Sistla, R., et al.: J. Pharm. Biomed. Anal., 39, 517 (2005),<br></p>

<p>Applications Tirofiban intermediate.<br></p>

<p>Impurity Nadolol EP Impurity B<br>Stability Hygroscopic<br>Applications (2R,3S)-rel-Nadolol-de(N-tert-butyl)methoxy 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>Stability Hygroscopic<br>Applications An active carboxylate of Mevastatin (M340500). It is a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A reductase with hypocholesterolemic activity. It has been shown to be effective in reducing cholesterol synthesis in vivo, and thereby in lowering cholesterol levels in blood.<br>References Endo, A. et al.: Atheroscler. Supp., 5, 39 (2004); Hosobuchi, M. et al.: J. Ferm. Bioeng., 76, 470 (1993);<br></p>

<p>Impurity Carvedilol EP Impurity C; Carvedilol Impurity C; Carvedilol USP C<br>Applications N-Benzyl Carvedilol (Carvedilol EP Impurity C) is an impurity of Carvedilol (C184625) and a degradation product in Carvedilol tablets.<br>References Karle, C., et al.: Cardiovasc. Res., 49, 361 (2001), Chen, J., et al.: Acta Cardiol. Sin., 19, 93 (2003), Xiang, T., et al.: Pharm. Res., 22, 1205 (2005),<br></p>

<p>Applications 3-(9H-Carbazol-4-yloxy)-1,2-propanediol is used in the synthesis of carvedilol, a β-adrenergic blocking agent.<br>References Naidu, K. et al.: Org. Chem. An Indian J., 6, 171 (2010);<br></p>

<p>Impurity Bisoprolol EP Impurity L (Metoprolol EP Impurity C)<br>Stability Hygrscopic<br>Applications 4-[2-Hydroxy-3-[(1-methylethyl)amino]propoxy]benzaldehyde (Bisoprolol EP Impurity L (Metoprolol EP Impurity C)) is a Metoprolol impurity .<br>References Baldwin, J.J. , et al.: J. Med. Chem., 29, 1065 (1986), Ravelet, C., et al.: J. Sep. Sci., 29, 1322 (2006),<br></p>

<p>Impurity Nicardipine USP Related Compound B<br>Applications A pyridine metabolite M-5 of Nicardipine. Nicardipine USP Related Compound B.<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 Triggle, A., et al.: J. Med. Chem., 23, 1442 (1980), Freedman, D., et al.: Drugs, 34, 578 (1987), Guengerich, F., et al.: Xenobiotica, 25, 689 (1995), Schleifer, K., et al.: Pharmazie, 54, 804 (1999),<br></p>

<p>Stability Light Sensitive<br>Applications Ciprofibrate Ethyl Ester is an impurity of ciprofibrate(C482475) is a hypolipemic agent, related structurally to Clofibrate (C586910). Ciprofibrate is used as an antilipemic.<br>References Davison, C., et al.: Drug. Metab. Dispos., 3, 520 (1975), Arnold, A., et al.: J. Pharm. Sci., et al.: 68, 1557 (1979), Tuchman-Duplessis, H., et al.: Toxicology, 12, 1 (1979),<br></p>

<p>Stability Hygroscopic<br>Applications An intermediate in the production of Rosuvastatin (R700500) derivatives.<br></p>

<p>Applications A metabolite of Carvedilol (C184625).<br>References McGurk, K., et al.: Biochem. Pharmacol., 55, 1005 (1998), Tukey, R., et al.: Annu. Rev. Pharmacol. Toxicol., 40, 581 (2000), Bowalgaha, K., et al.: Br. J. Clin. Pharmacol., 52, 605 (2001), Richardson, T., et al.: Drug Metab. Dispos., 34, 351 (2006),<br></p>

<p>Applications 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 Edoxaban is an anticoagulant drug which acts as a direct factor Xa inhibitor.<br>References Ruff, C., et al.: Am. Heart J., 160, 635 (2010); Ogata, K., et al.: J. Clin. Pharm., 50, 73 (2010)<br></p>

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

<p>Impurity Tranexamic EP Impurity A<br>Applications Tranexamic Acid Dimer (Tranexamic EP Impurity A) is a Tranexamic Acid (T714505) impurity.<br></p>

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

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

<p>Stability Hygroscopic<br>Applications 2'-(2H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-carboxylic Acid is a transformation product of Valsartan (V095750); a nonpeptide angiotensin II AT1-receptor antagonist and antihypertensive. 2'-(2H-Tetrazol-5-yl)-[1,1'-biphenyl]-4-carboxylic Acid is also referred to as Valsartan acid.<br>References Noedler, K., et al.: Water Res., 47, 6650 (2013); Criscione, L., et al.: Brit. J. Pharmacol., 110, 761 (1993); Muller, P., et al.: Eur. J. Clin. Pharmacol., 47, 231 (1994)<br></p>

<p>Impurity Rosuvastatin EP Impurity C (Calcium Salt)<br>Stability Hygroscopic<br>Applications 5-Oxo Rosuvastatin (Rosuvastatin EP Impurity C (Calcium Salt)) is a Rosuvastatin (R700500) impurity.<br>References Endo, A., et al.: J. Antibiot., 32, 852 (1979), Beck, G., et al.: J. Med. Chem., 33, 52 (1990), Koga, T., et al.: Lipids, 30, 775 (1995),<br></p>

<p>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.</p>

<p>4-(2-Methoxyethyl)phenol is a synthetic compound that is an antihypertensive agent. It is used to reduce high blood pressure, which may be due to its ability to block the action of angiotensin II, a potent vasoconstrictive hormone, by binding with its receptor. 4-(2-Methoxyethyl)phenol has been shown to be more potent than metoprolol succinate and less toxic than hydroxylated compounds such as propranolol in pharmacokinetic studies. In addition, 4-(2-Methoxyethyl)phenol has been found to have a low risk of congestive heart failure. The industrial process for this substance involves the reaction of hydrochloric acid with phenol in the presence of a catalyst such as aluminium chloride or zinc chloride.</p>

<p>3-[4-(2-Methoxyethyl)phenoxy]-1,2-propanediol is a synthetic intermediate. It is metabolized from the drug product 3-[4-(2-Methoxyethyl)phenoxy]propionic acid and may be used as an impurity standard for this compound. This chemical is a high purity, pharmacopoeia grade material that is suitable for use in drug development and pharmaceutical research. 3-[4-(2-Methoxyethyl)phenoxy]-1,2-propanediol has a natural origin and can be produced synthetically or through biotransformation of other compounds.</p>

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

<p>Penbutolol sulfate ((-)-Terbuclomine) is able to bind to both β2-adrenergic receptor and β1-adrenergic receptor, thus making it a non-selective β blocker.</p>

<p>Esmolol is a cardioselective beta-blocker used in parenteral forms in the treatment of arrhythmias and severe hypertension.</p>

<p>Applications Methyl 4-Hydroxyphenylacetate has been shown to have potent inhibitory activity against tobacco mosaic virus (TMV).<br>References Shen, S., Li, W., Wang, J.: Nat. Prod. Res., 27, 2286 (2013); Golovleva, L.A., et. al.:<br></p>

<p>Applications CMPD101 is a potent and selective GRK2/3 inhibitor.<br>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<br></p>