Bêta-bloquants

<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>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>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>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>Esmolol is a cardioselective beta-blocker used in parenteral forms in the treatment of arrhythmias and severe hypertension.</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>Applications A metabolite of Propranolol.<br>References Otton, S., et al.: Br. J. Clin. Pharmacol., 30, 751 (1990), Fujita, S., et al.: J. Pharmacol. Exp. Ther., 264, 226 (1993), Bichara, N., et al.: Drug Metab. Dispos., 24, 112 (1996), Tasaki, T., et al.: J. Biochem., 123, 162 (1998),<br></p>

<p>Applications 4-Hydroxy Flecainide is an analogue of Flecainide (F390000).<br>References Blom, Y., et al.: J. Chromatogr., 653, 138 (1993),<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 (S)-(-)-Hydroxy Timolol is a metabolite of the non-selective beta-adrenergic receptor blocker, Timolol (T443710).<br>References Volotinen, M. et al.: Basic Clin. Pharmacol. Toxicol., 106, 302 (2010);<br></p>

<p>Applications (S)-4-Hydroxy Propranolol is the main metabolite of (S)-Propranolol (P831795).<br>References Shwed, J., et al.: Xenobiotica, 22, 973 (1992), Fujita, K., et al.: Biol. Pharm. Bull., 22, 446 (1999), Walle, U., et al.: Drug Metab. Dispos., 30, 564 (2002),<br></p>

<p>Applications Rescinnamine is an angiotensin-converting enzyme inhibitor used as an antihypertensive drug.<br>References Fife, R., et al.: Brit. Med. J., 2, 1848 (1960); Balsevich, J., et al.: Planta Med., 44, 91 (1982)<br></p>

<p>Applications Lodoxamide-15N2,d2 is the labelled form of Lodoxamide which is an antiallergic drug that acts as a mast cell stabilizer. It is effective in the treatment of allergic conjunctivitis and in decreasing vascular permeability.<br>References Ciprandi, G., et al.: Allergy, 51(12), 946-951 (1996); Bayer, Atilla., et al.: Ophthalmologica, 217(2), 119-123 (2003)<br></p>

<p>Impurity Atorvastatin 2-Hydroxy Lactone<br>Stability Hygroscopic<br>Applications A metabolite of Atorvastatin, a selective, competitive HMG-CoA reductase inhibitor. Atorvastatin is the only drug in its class specfically indicated for lowering both elevated LDL-cholesterol and triglycerides in patients with hypercholesterolemia.<br></p>

<p>Applications Used as an antihypertensive and antianginal.<br>References Gross, G.J., et al.: Gen. Pharmacol., 14, 677 (1983), Molyvdas, P.A. and Sperelakis, N.: J. Cardiovasc. Pharmacol., 8, 449 (1986), Mizuno, K., et al.: Res. Comm. Chem. Pathol. Pharmacol., 52, 3 (1986)<br></p>