Title: Flunarizine
CAS Registry Number: 52468-60-7
CAS Name: (E)-1-[Bis(4-fluorophenyl)methyl]-4-(3-phenyl-2-propenyl)piperazine
Additional Names: (E)-1-[bis(p-fluorophenyl)-methyl]-4-cinnamylpiperazine; 1-cinnamyl-4-(di-p-fluorobenzhydryl)piperazine
Molecular Formula: C26H26F2N2
Molecular Weight: 404.49
Percent Composition: C 77.20%, H 6.48%, F 9.39%, N 6.93%
Literature References: Calcium channel blocker; fluorinated deriv of cinnarizine, q.v. Prepn: P. A. J. Janssen, DE 1929330 and FR 2014487; idem, US 3773939 (1970, 1970, 1973, all to Janssen). Pharmacology: L. K. Desmedt et al., Arzneim.-Forsch. 25, 1408 (1975); T. Godfraind, Eur. J. Pharmacol. 53, 273 (1979). Clinical studies: J. Schetz et al., Curr. Ther. Res. 23, 131 (1978); G. Rudofsky et al., Angiology 30, 479 (1979). Rheological effects in humans: J. D. Cree et al., ibid. 505. Mechanism of calcium blocking activity: T. Godfraind, Fed. Proc. 40, 2866 (1981). Clinical study in retinal vasculopathy: P. Nihard, Angiology 33, 37 (1982). Clinical trial in chronic cerebrovascular disorders: A. Agnoli et al., Int. J. Clin. Pharmacol. Res. 8, 189 (1988). Series of articles on absorption, distribution, excretion and metabolism: Arzneim.-Forsch. 33, 1135-1151 (1983). Review of pharmacology, toxicology and clinical studies: B. Holmes et al., Drugs 27, 6 (1984).
Derivative Type: Dihydrochloride
CAS Registry Number: 30484-77-6
Trademarks: Dinaplex (Sidus); Flugeral (Italfarmaco); Flunagen (Gentili); Flunarl (Kyowa Hakko); Fluxarten (SKB); Gradient (Polifarma); Issium (Lifepharma); Mondus (Labinca); Sibelium (Janssen)
Molecular Formula: C26H26F2N2.2HCl
Molecular Weight: 477.42
Percent Composition: C 65.41%, H 5.91%, F 7.96%, N 5.87%, Cl 14.85%
Properties: Crystals from a mixture of 2-propanol/ethanol, mp 251.5°.
Melting point: mp 251.5°
Therap-Cat: Vasodilator (cerebral and peripheral).
Keywords: Calcium Channel Blocker; Piperazine Derivatives; Vasodilator (Cerebral); Vasodilator (Peripheral). |