2820. Dapiprazole

Nomenclature

CAS number: 72822-12-9
5,6,7,8-Tetrahydro-3-[2-[4-(2-methylphenyl)-1-piperazinyl]ethyl]-1,2,4-triazolo[4,3-a]pyridine; 5,6,7,8-tetrahydro-3-[2-(4-o-tolyl-1-piperazinyl)ethyl]-s-triazolo[4,3-a]pyridine.
C19H27N5; mol wt 325.45.
C 70.12%, H 8.36%, N 21.52%.

Description and references

α-Adrenergic blocker. Prepn: B. Silvestrini, L. Baiocchi, DE 2915318; eidem, US 4252721 (1979, 1981 both to Angelini Francesco). Series of articles on general pharmacology: Arzneim.-Forsch. 32, 674-681 (1982); and toxicity: B. Silvestrini et al., ibid. 668. Ocular pharmacokinetics in rabbits: P. Valeri et al., Pharmacol. Res. Commun. 18, 1093 (1986). Topical effects in human eye: A. Reibaldi et al., Acta Ther. 10, 381 (1984); C. Malpassi et al., ibid. 12, 55 (1986). Clinical trial in reversal of mydriasis: R. W. Allinson et al., Ann. Ophthalmol. 22, 131 (1990).

Chemical structure

Properties

mp 158-160°.

Derivative

Monohydrochloride.

Nomenclature

CAS number: 72822-13-0
AF-2139; Glamidolo (Angelini); Reversil (Angelini); Rev-Eyes (Angelini).
C19H27N5.HCl; mol wt 361.91.
C 63.06%, H 7.80%, N 19.35%, Cl 9.80%.

Properties

Crystals from absolute ethanol, mp 206-207°. LD50 in mice (mg/kg): 260 i.p. (Silvestrini).

Therapeutic Category

Antiglaucoma; miotic.

Keywords

α-Adrenergic Blocker; Antiglaucoma