7813. Propentofylline

Nomenclature

CAS number: 55242-55-2
3,7-Dihydro-3-methyl-1-(5-oxohexyl)-7-propyl-1H-purine-2,6-dione; 3-methyl-1-(5-oxohexyl)-7-propylxanthine; 1-(5′-oxohexyl)-3-methyl-7-propylxanthine; HWA-285; Albert-285; HOE-285; Hextol (Hoechst); Karsivan (Provet).
C15H22N4O3; mol wt 306.36.
C 58.81%, H 7.24%, N 18.29%, O 15.67%.

Description and references

Peripheral vasodilator which inhibits cyclic AMP phosphodiesterase. Prepn: W. Mohler et al., DE 2330742; eidem, US 4289776 (1975, 1981 both to Hoechst). Cardiovascular effects in animals: O. Hudlicka et al., Br. J. Pharmacol. 72, 723 (1981). Effect on cAMP phosphodiesterase: K. Nagata et al., Arzneim.-Forsch. 35, 1034 (1985). Inhibition of adenosine uptake: B. B. Fredholm, K. Lindstr"om, Acta Pharmacol. Toxicol. 58, 187 (1986). Cerebrovascular effects in animals: J. J. Grome et al., Drug Dev. Res. 5, 111 (1985). Effect on postischemic brain edema: B. B. Mrsulja et al., ibid. 6, 339 (1985). Effect on cognitive function in humans: I. Hindmarch, Z. Subhan, ibid. 5, 379 (1985). Acute toxicity: M. Inazu et al., Oyo Yakuri 31, 357 (1986), C.A. 104, 218960a (1986).

Chemical structure

Properties

Crystals from diisopropyl ether, mp 69-70°. Soly in water at 25°: 3.2%; in ethanol: >10%; in DMSO: >10%. LD50 in male, female mice, male, female rats (mg/kg): 900, 780, 1150, 940 orally; 168, 170, 180, 195 i.v.; 375, 346, 199, 196 i.p.; 450, 508, 400, 338 s.c. (Inazu).

Therapeutic Category

Nootropic.

Therapeutic Category (Veterinary)

Vasodilator (peripheral and cerebral).

Keywords

Nootropic