Title: Ibudilast
CAS Registry Number: 50847-11-5
CAS Name: 2-Methyl-1-[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]-1-propanone
Additional Names: 3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine
Manufacturers' Codes: KC-404
Trademarks: Ketas (Kyorin)
Molecular Formula: C14H18N2O
Molecular Weight: 230.31
Percent Composition: C 73.01%, H 7.88%, N 12.16%, O 6.95%
Literature References: Leukotriene D4 antagonist. Prepn: T. Irikura et al., DE 2315801; eidem, US 3850941 (1973, 1974 both to Kyorin). Pharmacology and antiallergic activity: K. Nishino et al., Jpn. J. Pharmacol. 33, 267 (1983); H. Nagai et al., ibid. 1215. In vitro cerebral vasodilating activity: M. Ohashi et al., Arch. Int. Pharmacodyn. 280, 216 (1986); in vivo activity: W. M. Armstead et al., J. Pharmacol. Exp. Ther. 244, 138 (1988). Bronchodilating activity in animals: S. Mue et al., Arch. Int. Pharmacodyn. 283, 153 (1986). Antiplatelet activity in animals: M. Ohashi et al., ibid. 321; M. Ohashi et al., Gen. Pharmacol. 17, 385 (1986).
Properties: Crystals from hexane, mp 53.5-54°. Slightly sol in water, freely sol in organic solvents. LD50 i.v. in mice: 260 mg/kg (Irikura, 1973).
Melting point: mp 53.5-54°
Toxicity data: LD50 i.v. in mice: 260 mg/kg (Irikura, 1973)
Therap-Cat: Antiallergic; antiasthmatic; vasodilator (cerebral).
Keywords: Antiallergic; Antiasthmatic (Nonbronchodilator); Leukotriene Antagonist; Vasodilator (Cerebral). |