Title: Lomerizine
CAS Registry Number: 101477-55-8
CAS Name: 1-[Bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]piperazine
Additional Names: 1-[bis(p-fluorophenyl)methyl]-4-(2,3,4-trimethoxybenzyl)piperazine; 1-(2,3,4-trimethoxybenzyl)-4-[bis(4-fluorophenyl)methyl]piperazine
Molecular Formula: C27H30F2N2O3
Molecular Weight: 468.54
Percent Composition: C 69.21%, H 6.45%, F 8.11%, N 5.98%, O 10.24%
Literature References: Diphenylpiperazine calcium channel blocker; selective cerebral vasodilator. Prepn: H. Ohtaka et al., EP 159566; eidem, US 4663325 (1985, 1987 both to Kanebo); eidem et al., Chem. Pharm. Bull. 35, 3270 (1987). Structure-activity study: H. Ohtaka, G. Tsukamoto, ibid. 4117. HPLC determn in plasma and brain tissue: H. Waki, S. Ando, J. Chromatogr. 494, 408 (1989). Pharmacology: T. Kanazawa et al., J. Cardiovasc. Pharmacol. 16, 430 (1990). Protective effect in cerebral ischemia: H. Hara et al., Arch. Int. Pharmacodyn. 304, 206 (1990); V. Danielisova, M. Chavko, Neurochem. Res. 19, 1503 (1994).
Derivative Type: Dihydrochloride
CAS Registry Number: 101477-54-7
Manufacturers' Codes: KB-2796
Trademarks: Terranas (Nippon Organon)
Molecular Formula: C27H30F2N2O3.2HCl
Molecular Weight: 541.46
Percent Composition: C 59.89%, H 5.96%, F 7.02%, N 5.17%, O 8.86%, Cl 13.10%
Properties: Colorless crystals from acetonitrile, mp 214-218° (dec). Also reported as mp 204-207° (dec). LD50 orally in mice: 300 mg/kg (Ohtaka).
Melting point: mp 214-218° (dec); mp 204-207° (dec)
Toxicity data: LD50 orally in mice: 300 mg/kg (Ohtaka)
Therap-Cat: Antimigraine.
Keywords: Antimigraine; Calcium Channel Blocker; Piperazine Derivatives; Vasodilator (Cerebral). |