301. Almitrine

Nomenclature

CAS number: 27469-53-0
6-[4-[Bis(4-fluorophenyl)methyl]-1-piperazinyl]-N2,N4-di-2-propen-1-yl-1,3,5-triazine-2,4-diamine; 2,4-bis[allylamino]-6-[4-[bis(p-fluorophenyl)methyl]-1-piperazinyl]-s-triazine; S-2620.
C26H29F2N7; mol wt 477.55.
C 65.39%, H 6.12%, F 7.96%, N 20.53%.

Description and references

Prepn: G. Regnier, R. Canevari, DE 1947332; eidem, US 3647794 (1970, 1972 both to Sci. Union et Cie.-Soc. Fran. Recher. Méd.). Physical properties and toxicity: G. Regnier et al., Experientia 28, 814 (1972). Pharmacology: M. Laubie, F. Diot, J. Pharmacol. 3, 363 (1972); M. Laubie, H. Schmitt, Eur. J. Pharmacol. 61, 125 (1980). Evaluation of combination with raubasine, q.v., in cerebral ischemia in rats: M. G. Borzeix, J. Cahn, Arzneim.-Forsch. 37, 491 (1987). Clinical effect on hypoxemia in chronic obstructive pulmonary disease: R. C. Bell et al., Ann. Intern. Med. 105, 342 (1986); B. Gothe et al., Am. J. Med. 84, 436 (1988).

Chemical structure

Properties

Crystals, mp 181°.

Derivative

Dimethanesulfonate.

Nomenclature

CAS number: 29608-49-9
Almitrine dimesylate; Vectarion (Servier).
C26H29F2N7.2CH3SO3H; mol wt 669.76.
C 50.21%, H 5.57%, F 5.67%, N 14.64%, S 9.58%, O 14.33%.

Properties

mp 243° (dec). uv max (ethanol): 227, 246 nm (log ε 4.52, 4.53). LD50 in mice: 210 mg/kg i.v., 390 mg/kg i.p., >2 g/kg orally (Regnier).

Therapeutic Category

Respiratory stimulant.

Keywords

Respiratory Stimulant