Amosulalol
Title: Amosulalol
CAS Registry Number: 85320-68-9
CAS Name: 5-[1-Hydroxy-2-[[2-(2-methoxyphenoxy)ethyl]amino]ethyl]-2-methylbenzenesulfonamide
Molecular Formula: C18H24N2O5S
Molecular Weight: 380.46
Percent Composition: C 56.82%, H 6.36%, N 7.36%, O 21.03%, S 8.43%
Literature References: Sulfonamide-substituted phenylethanolamine with a- and b-adrenergic blocking activity. Prepn: K. Imai et al., DE 2843016; eidem, US 4217305 (1979, 1980 both to Yamanouchi). Pharmacology and receptor blocking activity: T. Takenaka et al., Eur. J. Pharmacol. 85, 35 (1982); of isomers: K. Honda et al., J. Pharmacol. Exp. Ther. 236, 776 (1986). GC determn in urine: H. Kamimura et al., J. Chromatogr. 275, 81 (1983); HPLC determn in plasma: H. S. Gwak et al., J. Chromatogr. B 818, 109 (2005). Clinical pharmacokinetics: M. Nakashima et al., Clin. Pharmacol. Ther. 36, 436 (1984); metabolism: H. Kamimura et al., Xenobiotica 15, 413 (1985). Clinical evaluation in hypertension: K. Ando et al., J. Cardiovasc. Pharmacol. 20, 7 (1992).
 
Derivative Type: Monohydrochloride
CAS Registry Number: 93633-92-2
Manufacturers' Codes: YM-09538
Trademarks: Lowgan (Yamanouchi)
Molecular Formula: C18H24N2O5S.HCl
Molecular Weight: 416.92
Percent Composition: C 51.85%, H 6.04%, N 6.72%, O 19.19%, S 7.69%, Cl 8.50%
Properties: Colorless crystals, mp 158-160°. pK1 7.4; pK2 10.2.
Melting point: mp 158-160°
pKa: pK1 7.4; pK2 10.2
 
Derivative Type: R-(-)-Form hydrochloride
Properties: mp 158°. [a]D20 -30.4° (c = 1 in methanol).
Melting point: mp 158°
Optical Rotation: [a]D20 -30.4° (c = 1 in methanol)
 
Derivative Type: S-(+)-Form hydrochloride
Properties: mp 158°. [a]D20 +30.7° (c = 1 in methanol).
Melting point: mp 158°
Optical Rotation: [a]D20 +30.7° (c = 1 in methanol)
 
Therap-Cat: Antihypertensive.
Keywords: a-Adrenergic Blocker; ?Adrenergic Blocker; Antihypertensive; Arylethanolamine Derivatives.

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