Title: Arotinolol
CAS Registry Number: 68377-92-4
CAS Name: 5-[2-[[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropyl]thio]-4-thiazolyl]-2-thiophenecarboxamide
Additional Names: 2-(3¢-tert-butylamino-2¢-hydroxypropylthio)-4-(5¢-carbamoyl-2¢-thienyl)thiazole
Molecular Formula: C15H21N3O2S3
Molecular Weight: 371.54
Percent Composition: C 48.49%, H 5.70%, N 11.31%, O 8.61%, S 25.89%
Literature References: Propanolamine deriv with a- and b-adrenergic blocking activity. Prepn: T. Hibino et al., DE 2341753; eidem, US 3932400 (1974, 1976 both to Sumitomo); Y. Hara et al., J. Pharm. Sci. 67, 1334 (1978). Characterization of adrenoceptor blocking effects in vivo: A. Miyagishi et al., Arch. Int. Pharmacodyn. Ther. 271, 249 (1984). Possible antianginal effects: M. Sakanashi et al., Oyo Yakuri 28, 709 (1984); C.A. 102, 39669z (1985). Long-term antihypertensive effect in rats: K. Kishi et al., J. Pharmacobio-Dyn. 8, 50 (1985). Comparison with timolol, q.v., of effect on intraocular pressure and hemodynamics: M. Nakashima et al., Eur. J. Clin. Pharmacol. 28, 391 (1985).
Properties: Crystals from chloroform/petroleum ether, mp 148-149°.
Melting point: mp 148-149°
Derivative Type: Hydrochloride
CAS Registry Number: 68377-91-3
Manufacturers' Codes: S-596; ARL
Trademarks: Almarl (Sumitomo)
Molecular Formula: C15H21N3O2S3.HCl
Molecular Weight: 408.00
Percent Composition: C 44.16%, H 5.43%, N 10.30%, O 7.84%, S 23.58%, Cl 8.69%
Properties: Crystals from methanol/water, mp 234-235.5° (dec). LD50 in mice (mg/kg): 86 i.v., >360 i.p., >5000 orally (Hara).
Melting point: mp 234-235.5° (dec)
Toxicity data: LD50 in mice (mg/kg): 86 i.v., >360 i.p., >5000 orally (Hara)
Therap-Cat: Antihypertensive; antianginal; antiarrhythmic.
Keywords: a-Adrenergic Blocker; ?Adrenergic Blocker; Antianginal; Antiarrhythmic; Antihypertensive; Aryloxypropanolamine Derivatives. |