3428. Dotarizine

Nomenclature

CAS number: 84625-59-2
1-(Diphenylmethyl)-4-[3-(2-phenyl-1,3-dioxolan-2-yl)propyl]piperazine; FI-6026.
C29H34N2O2; mol wt 442.59.
C 78.70%, H 7.74%, N 6.33%, O 7.23%.

Description and references

Mixed calcium channel blocker and serotonin (5-HT2) receptor antagonist. Prepn: R. Foguet et al., EP 97340; eidem, US 4883797 (1984, 1989 both to Ferrer); S. Gubert et al., Arzneim.-Forsch. 37, 1103 (1987). Clinical pharmacokinetics and tolerability: M. Farré et al., Methods Find. Exp. Clin. Pharmacol. 19, 343 (1997). Cerebrovascular study in goats: G. Torregrosa et al., Arzneim.-Forsch. 49, 668 (1999); in rabbits: N. Kuridze et al., J. Neurol. Sci. 175, 13 (2000). Mechanism of blockade: A. Ruiz-Nuno et al., Eur. J. Pharmacol. 411, 289 (2001).

Chemical structure

Properties

White crystalline solid from methanol, mp 100-101° (Gubert); also reported as 93-97° (Foguet).

Therapeutic Category

Antimigraine.

Keywords

Calcium Channel Blocker; Piperazine Derivatives; Serotonin Receptor Antagonist; Antimigraine