Mibefradil
Title: Mibefradil
CAS Registry Number: 116644-53-2
CAS Name: Methoxyacetic acid (1S,2S)-2-[2-[[3-(1H-benzimidazol-2-yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenyl ester
Additional Names: (1S,2S)-2-[2-[[3-(2-benzimidazolyl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphthyl methoxyacetate
Molecular Formula: C29H38FN3O3
Molecular Weight: 495.63
Percent Composition: C 70.28%, H 7.73%, F 3.83%, N 8.48%, O 9.68%
Literature References: Selective T-type calcium channel blocker. Prepn: Q. Branca et al., EP 268148; eidem, US 4808605 (1988, 1989 both to Hoffmann-La Roche). Calcium channel selectivity: S. K. Mishra, K. Hermsmeyer, Circ. Res. 75, 144 (1994). Metabolism in rats: H. R. Wiltshire et al., Xenobiotica 22, 837 (1992). Review of pharmacology, toxicology and clinical evaluation: J.-P. Clozel et al., Cardiovasc. Drug Rev. 9, 4-17 (1991); of pharmacology and pharmacokinetics: D. R. Abernethy, Am. J. Cardiol. 80, 4C-11C (1997); of clinical trials in hypertension: S. Oparil, Am. J. Hypertens. 11, 88S-94S (1998); in chronic stable angina pectoris: B. M. Massie, ibid. 95S-102S. Post-marketing safety assessment: J. Riley et al., Int. J. Clin. Pharmacol. Ther. 40, 241 (2002).
 
Derivative Type: Dihydrochloride
CAS Registry Number: 116666-63-8
Manufacturers' Codes: Ro-40-5967
Trademarks: Posicor (Roche)
Molecular Formula: C29H38FN3O3.2HCl
Properties: Bitter tasting, odorless, white crystalline powder, mp 128°. Chemically stable, light insensitive and water soluble. pKa: 4.8; 5.5. LD50 in mice, rats (mg/kg): 35, 23 i.v.; >800, >800 orally (Clozel).
Melting point: mp 128°
pKa: pKa: 4.8; 5.5
Toxicity data: LD50 in mice, rats (mg/kg): 35, 23 i.v.; >800, >800 orally (Clozel)
 
Therap-Cat: Antihypertensive.
Keywords: Antihypertensive; Calcium Channel Blocker; Arylalkylamines.

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