Title: Losartan
CAS Registry Number: 114798-26-4
CAS Name: 2-Butyl-4-chloro-1-[[2¢-(1H-tetrazol-5-yl)[1,1¢-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol
Additional Names: 2-n-butyl-4-chloro-5-hydroxymethyl-1-[[2¢-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]imidazole; 2-butyl-4-chloro-1-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]imidazole-5-methanol
Molecular Formula: C22H23ClN6O
Molecular Weight: 422.91
Percent Composition: C 62.48%, H 5.48%, Cl 8.38%, N 19.87%, O 3.78%
Literature References: Non-peptide angiotensin II receptor antagonist. Prepn: D. J. Carini, J. J. V. Duncia, EP 253310; D. J. Carini et al, US 5138069 (1988, 1992 both to Du Pont); D. J. Carini et al., J. Med. Chem. 34, 2525 (1991). Angiotensin receptor binding study: A. T. Chiu et al., J. Pharmacol. Exp. Ther. 252, 711 (1990); receptor subtype specificity: A. T. Chiu et al., Biochem. Biophys. Res. Commun. 172, 1195 (1990). Pharmacology of active metabolite, EXP-3174: P. C. Wong et al., J. Pharmacol. Exp. Ther. 255, 211 (1990). Symposium on pharmacology: Am. J. Hypertens. 4, 271S-353S (1991). Review of clinical experience in hypertension: M. McIntyre et al., Pharmacol. Ther. 74, 181-194 (1997). Clinical effect on mortality in heart failure: B. Pitt et al., Lancet 355, 1582 (2000). Renoprotective effect in diabetic nephropathy: B. M. Brenner et al., N. Engl. J. Med. 345, 861 (2001).
Properties: Light yellow solid, mp 183.5-184.5°. pKa: 5-6.
Melting point: mp 183.5-184.5°
pKa: pKa: 5-6
Derivative Type: Monopotassium salt
CAS Registry Number: 124750-99-8
Manufacturers' Codes: Du Pont 753; DUP-753; MK-954
Trademarks: Cozaar (DuPont); Lortaan (Merck & Co.); Lorzaar (Merck & Co.); Losaprex (Sigma-Tau); Neo-Lotan (Neopharmed)
Molecular Formula: C22H22ClKN6O
Molecular Weight: 461.00
Percent Composition: C 57.32%, H 4.81%, Cl 7.69%, K 8.48%, N 18.23%, O 3.47%
Derivative Type: Monopotassium salt mixture with hydrochlorothiazide
Trademarks: Fortzaar (DuPont); Hyzaar (DuPont)
Therap-Cat: Antihypertensive.
Keywords: Angiotensin II Receptor Antagonist; Antihypertensive; Biphenyltetrazole Derivatives. |