3942. Fasudil
Nomenclature
CAS number: 103745-39-7
Hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine; N-(5-isoquinolinesulfonyl)-1,4-perhydrodiazepine; 1-(5-isoquinolinesulfonyl)homopiperazine. C14H17N3O2S; mol wt 291.37.
C 57.71%, H 5.88%, N 14.42%, O 10.98%, S 11.00%.
Description and references
Intracellular calcium antagonist. Prepn: H. Hidaka, T. Sone, EP 187371; eidem, US 4678783 (1986, 1987 both to Asahi); A. Morikawa et al., Chem. Pharm. Bull. 40, 770 (1992). Pharmacology: T. Asano et al., Br. J. Pharmacol. 98, 1091 (1989). Mechanism of action: idem et al., J. Pharmacol. Exp. Ther. 241, 1033 (1987). Clinical trials: M. Shibuya et al., J. Neurosurg. 76, 571 (1992). Acute toxicity: H. Koga et al., Yakuri to Chiryo 20, S1433 (1992), C.A. 117, 226005b (1992). Review of pharmacology and clinical evaluation: M. Shirotani et al., Cardiovasc. Drug Rev. 10, 333-357 (1992).
Derivative
Hydrochloride.Nomenclature
CAS number: 105628-07-7
AT-877; HA-1077; Eril (Asahi). C14H17N3O2S.HCl; mol wt 327.83.
C 51.29%, H 5.53%, N 12.82%, O 9.76%, S 9.78%, Cl 10.81%.
Properties
Crystals from water, mp 220.5°. Also reported as white crystalline powder, mp 219.3° (Shirotani). Sol in water up to 2 × 10-2M at pH 5.0-7.0. LD50 in mice, rats (mg/kg): 67.5, 59.9 i.v.; 124.5, 123.2 s.c.; 273.9, 335.0 orally (Koga).Therapeutic Category
Vasodilator (cerebral).
Keywords
Vasodilator (Cerebral)