9173. Tertatolol

Nomenclature

CAS number: 34784-64-0
1-[(3,4-Dihydro-2H-1-benzothiopyran-8-yl)oxy]-3-[(1,1-dimethylethyl)amino]-2-propanol; (±)-1-tert-butylamino-3-(1-thiachroman-8-yloxy)-2-propanol; dl-8-[2-hydroxy-3-[(tert-butylamino)propyl]oxy]thiochromane.
C16H25NO2S; mol wt 295.44.
C 65.05%, H 8.53%, N 4.74%, O 10.83%, S 10.85%.

Description and references

Nonselective β-adrenergic blocker. Prepn: C. Malen, M. Laubie, DE 2115201; eidem, US 3960891 (1971, 1976 both to Sci. Union et Cie). Pharmacology in animals: M. Laubie et al., Arch. Int. Pharmacodyn. Ther. 201, 323, 334 (1973); B. R. Walker et al., J. Cardiovasc. Pharmacol. 7, 1193 (1985). Synergistic effect with indapamide, q.v.: E. Marmo et al., Drugs Exp. Clin. Res. 11, 709 (1985). GC-MS determn in plasma and urine: S. Staveris et al., J. Chromatogr. 339, 97 (1985). Pharmacology in humans and mechanism of action study: A. De Blasi et al., Clin. Pharmacol. Ther. 39, 245 (1986). Preliminary evaluation in hypertension: J. P. Degaute et al., Am. J. Hypertens. 1, 263S (1988).

Chemical structure

Properties

Crystals from hexane, mp 70-72°.

Derivative

Hydrochloride.

Nomenclature

CAS number: 33580-30-2
S-2395; SE-2395; Artex (Servier); Artexal (Servier); Prenalex (Itherapia).
C16H25NO2S.HCl; mol wt 331.90.
C 57.90%, H 7.90%, N 4.22%, O 9.64%, S 9.66%, Cl 10.68%.

Properties

Crystals from acetonitrile, mp 180-183°. pKa 9.8. LD50 in rats, mice (mg/kg): 40, 37 i.v.; 90, 120 i.p. (Laubie).

Therapeutic Category

Antihypertensive.

Keywords

β-Adrenergic Blocker; Antihypertensive; Aryloxypropanolamine Derivatives