Beta Blockers

Applications Simvastatin-d6 Hydroxy Acid Sodium Salt is a labeled metabolite of Simvastin (S485000). A competitive inhibitor of HMG-CoA reductase. References Hoffman, W.F., et al.: J. Med. Chem., 29, 849 (1986); Mol, M.J., et al.: Lancet, 2, 936 (1986)

Applications A metabolite of Papaverine (P190500). 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 Wilen, G., et al.: J. Pharm. Phamacol., 34, 264 (1982), Cone, E., et al.: J. Anal. Toxicol., 15, 1 (1991), Staub, C., et al.: Clin. Chem., 47, 301 (2001),

Applications Labelled (R)-enantiomer of Metoprolol. An antihypertensive, though up to 380 times less potent than the (S)-enantiomer. References Toda, N., et al.: J. Pharm. Exp. Ther., 207, 311 (1978),

Applications CMPD101 is a potent and selective GRK2/3 inhibitor. 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

Stability Hygroscopic Applications α2-Adrenoceptor agonist related structurally to Clonidine. Used in treatment of opioid withdrawal symptoms; antihypertensive. 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 Velly, J., et al.: J. Pharmacol., 8, 351 (1977), Jarrot, B., et al.: Biochem. Pharmacol., 28, 141 (1979), Birch, P., at al.: Brit. J. Pharmacol., 68, 107 (1980),

Stability Hygroscopic Applications A isotopically labelled metabolite of Losartan, a nonpeptide angiotensin II AT1-receptor antagonist. References Pieter, B.M.W.M., et al.: Hypertension, Supp. III, 18, 5, (1991), Chang, L.L., et al.: J. Med. Chem., 36, 2558 (1993)

(R)-Propranolol hydrochloride (Dexpropranolol hydrochloride) is the less active enantiomer of the anti-adrenoceptor (β-adrenoceptor) antagonist propranolol.

Applications Atorvastatin (A791750) impurity. References Kearney, A.S., et al.: Pharm. Res., 10, 1461 (1993); Heinonen, T.M., et al.: Clin. Ther., 18, 853 (1996);

Stability Hygroscopic Applications rac-4-Hydroxy Propranolol Hydrochloride is a metabolite of Propranolol. 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),

Impurity Valsartan Related Compound B Applications Valsartan n-Propyl is an impurity in the synthesis of Valsartan (V095750). Valsartan USP Related Compound B. References Hillaert, S., et al.: J. Pharm. Biomed. Anal., 31, 329 (2003), Carlucci, G., et al.: Anal. Lett., 33, 2491 (2000), Cagigal, E., et al.: Talanta, 54, 1121 (2001),

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 A metabolite of Nisoldipine (N489125). References Grossi, P., et al.: Xenobiotica, 22, 899 (1992), Hayase, N., et al.: J. Pharm. Sci., 83, 532 (1994), Barlett, M., et al.: J. Pharm. Biomed. Anal., 18, 335 (1998), Nayler, W., et al.: J. Clin. Basic Cardiol., 2, 155 (1999), Mielcarek, J., et al.: J. Pharm. Biomed. Anal., 24, 71 (2000),

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

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),

Stability Very Hygroscopic Applications An arginine derivative; used in chronic kidney diseases.A potential endogenous nitric oxide inhibitor in dialysis. References Ogawa, T., et al.: J. Biol. Chem., 264, 10205 (1989), Boulanger, C., et al.: J. Clin. Invest., 85, 587 (1990), Alipui, C., et al.: J. Pharmacol. Methods, 26, 211 (1991), Azuma, H., et al.: Br. J. Pharmacol., 106, 665 (1992), Vallence, P., et al.: Lancet, 339, 572 (1992), Goto, M., et al.: J. Cardiovasc. Pharmacol., 41, 265 (2003),

Stability Hygroscopic 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. 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),