Beta Blockers

Applications Carvedilol-d5 is the labelled analog of Carvedilol, a nonselective β-adrenergic blocker with α1-blocking activity. Carvedilol is 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), Packer, M., et al.: N. Engl. J. Med., 334, 1349 (1996),

Applications Hydrochloride salt derivative of Dideiodo Amiodarone (D439420), an intermediate of Amiodarone (A632950). References Weir, S., et al.: J. Pharm. Sci., 74, 460 (1985), Ramanathan, R., et al.: Anal. Chem., 72, 1352 (2000),

Impurity Simvastatin Impurity K Applications 4α,5-Dihydro Simvastatin is an impurity in the synthesis of Simvastatin (S485000), 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. References Hoffman, W.F., et al.: J. Med. Chem., 29, 849 (1986), Mol, M.J., et al.: Lancet, 2, 936 (1986),

Applications A natural, active form of folic acid used at the cellular level for DNA reproduction, the cysteine cycle and the regulation of homocysteine among other functions. It is a coenzymated form of folic acid. It has been proposed for treatment of cardiovascular disease. References Willems, F. et al.: Br. J. Pharmacol., 145, 823 (2004); Prinz-Langhebohi, R.: et al., Br. J. Pharmacol., 158, 2014 (2009); Wright, A. et al.: Brit, J. Nutrit., 103, 724 (2010)

Applications A metabolite of Torsemide (T548750). References Besenfelder, E., et al.: J. Pharm. Biomed. Anal., 5, 259 (1987), Vormfelde, S., et al.: Clin. Pharmacol. Ther., 76, 557 (2004),

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

Stability Hygroscopic, Light Sensitive, Temperature Sensitive Applications An intermediate in the Maillard reaction of proteins with glucose, which is metabolised to 3-Deoxyfructose. An intermediate in the formation of pyrraline, which might contribute to a pathological effect, such as carcinogenesis. References Kato, H. et al.: Agric. Biol. Chem., 51, 683 (1987), Hayase, F. et al.: J. Biol. Chem., 264, 3758 (1989), Kato, H. et al.: Biochimica et Biophysica Acta, 1035, 71 (1990)

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