Bêta-bloquants

Applications Benzthiazide is a diuretic, antihypertensive agent. References Mollica, J., et al.: J. Pharm. Sci., 58, 635 (1969), Chienthavorn, O., et al.: J. Pharm. Biomed. Anal., 36, 477 (2004),

Applications A deuterated 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 Amiodarone, a non-selective ion channel blocker. References Ha, H., et al.: Eur. J. Clin. Pharmacol., 55, 807 (2000), Arai, K., et al.: J. Biochem., 132, 529 (2002), Carson, B., et al.: J. Med. Chem., 31, 623 (2002),

Impurity Nifedipine EP Impurity B Applications A photodegradation product of Nifedipine (N457000). Shown to relax contractions of the rat aortic strip induced by norepinephrine and other agonists. References Hayase, N. et at.: J. Pharmac. Exp. Ther., 275, 813 (1995); De Vries, H. et al.: Photochem. Photobio., 62, 959 (1995);

Penbutolol is a nonselective beta-blocker utilized as an antihypertensive and an antianginal.

Ether-alcohols and their halogenated, sulfonated, nitrated or nitrosated derivatives not elsewhere specified or included

Stability Hygroscopic Applications Atorvastatin impurity in bulk drug and tablets. References Posvar, E., et al.: J. Clin. Pharmacol., 36, 728 (1996), Lea, A., et al.: Drugs, 53, 828 (1997), Miao, X., et al.: J. Chromatogr., 998, 133 (2003),

Applications Propoxyphenyl Homohydroxysildenafil is an analogue of Homo Sildenafil (H615150) that may be used as a method for treating erectile dysfunction.

Applications The R-(+)-form of Warfarin (W498500). Coumarin anticoagulant. 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 Hagan, E.C., et al.: J. Am. Pharm. Assoc. Sci. Ed., 42, 379 (1953), Bell, R.G., et al.: Biochemistry, 11, 1959 (1972), Valente, J.E., et al.: J. Med. Chem., 20, 1489 (1977), Back, N., et al.: Pharmacol. Res. Commun., 10, 445, (1978), Babhair, S.A., et al.: Anal. Profiles Drug Subs., 14, 423 (1985), Takahashi, H., et al.: Echizen, Clin. Pharmacokinet., 40, 587 (2001),

Applications GBT 440 is a potent allosteric effector of sickle cell hemoglobin (Hb) that increases the affinity of Hb for oxygen and inhibits its polymerization when subjected to hypoxic conditions. References Metcalf, B., et al.: ACS Med. Chem., 8, 321-326 (2017); Li, Q., et al.: Proc. Natl. Acad. Sci. U.S.A., 114, E689-E696 (2017)

Applications An angiotensin II type 1 (AII1)-receptor antagonist. References Gillis, J.C. and Markham, A.: Drugs, 54, 885 (1997), Chando, T.J., et al.: Drug. Metabol. Dispos., 26, 408 (1998), Massie, B., et al.: New Eng. J. Med., 359, 2456 (2008), Ren, X., et al.: Pharmacol., 83, 80 (2009),

Impurity Simvastatin EP Impurity B Applications 4'-Acetyl Simvastatin (Simvastatin EP Impurity B) is a Simvastatin (S485000) impurity. References Shioi, A., et al.: J. Phys. Chem., 99, 4750 (1995), Wang, L., et al.: J. Pharm. Biomed. Anal., 21, 1243 (2000), Vuletic, M., et al.: J. Pharm. Biomed. Anal., 37, 715 (2005),

Applications An intermediate of Rosuvastatin (R700500).

Stability Hygroscopic Applications A competitive inhibitor of HMG-CoA reductase. Bioactive metabolite of Mevastatin. References Serizawa, N., et al.: J. Antibiot., 36, 604 (1983), Yoshino, G., et al.: Lancet, 2, 740 (1986), White, H.D, et al.: N. Engl. J. Med., 343, 317 (2000)

Aromatic drugs of amino-alcohols, other than those cont

Impurity Ezetimibe Ketone (USP) Applications Phase-I metabolite of Ezetimibe (E975000). 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),

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. References Caraci, F., et. al.: Brain Res., 1047, 30 (2005); Mizuno, T., et. al.: Brain Res., 1066, 78 (2005)

Applications Canadine is a protoberberine alkaloid which potently block functional KATP channels natively expressed on midbrain dopamine neurons. Canadine is used for treatment of degenerative diseases or conditions associated with KATP channel signaling. References Duchowicz, P., et al.: Bioorg. Med. Chem., 14, 5876 (2006), Sun., et al.: Br. J. Pharmcol., 158, 1302 (2009), Deeb, O., et al.: Chem. Biol. Drug Des., 76, 255 (2010),

Applications MMAE is an effective and synthetic cytotoxic analog of Dolastatin 10 which is a potent antimitotic polypeptide isolated from a marine animal. References Bai R. et al.: J. biol. Chem., 265, 17141 (1990); Giddens, A. et al.: Bioorg. Med. Chem., 24, 6075 (2016);