Title: Naftopidil
CAS Registry Number: 57149-07-2
CAS Name: 4-(2-Methoxyphenyl)-a-[(1-naphthalenyloxy)methyl]-1-piperazineethanol
Additional Names: RS-1-[4-(2-methoxyphenyl)-1-piperazinyl]-3-(1-naphthoxy)-2-propanol; 1-(2-methoxyphenyl)-4-[3-(naphth-1-yloxy)-2-hydroxypropyl]-piperazine
Manufacturers' Codes: KT-611
Trademarks: Avishot (Kanebo); Flivas (Asahi)
Molecular Formula: C24H28N2O3
Molecular Weight: 392.49
Percent Composition: C 73.44%, H 7.19%, N 7.14%, O 12.23%
Literature References: a1-Adrenergic blocker and serotonin (5HT1A) receptor agonist. Prepn: E. C. Witte et al., DE 2408804; eidem, US 3997666 (1975, 1976 both to Boehringer Mann.). Clinical pharmacodynamics: R. Kirsten et al., Eur. J. Clin. Pharmacol. 46, 271 (1994). Clinical pharmacokinetics: M. J. G. Farthing et al., Postgrad. Med. J. 70, 363 (1994). HPLC determn in human plasma: G. Niebch et al., J. Chromatogr. 534, 247 (1990). Clinical evaluation in BPH: K. Yasuda et al., Prostate 25, 46 (1994). Review of pharmacology and clinical experience: H. M. Himmel, Cardiovasc. Drug Rev. 12, 32-47 (1994).
Properties: Crystals from isopropanol, mp 125-126°; also reported as colorless crystals, mp 125-129°. Insol in water. Partition coefficient (octanol/water): 75. LD50 in mice, rats (g/kg): 1.3, 6.4 orally (Himmel).
Melting point: mp 125-126°; mp 125-129°
Log P: Partition coefficient (octanol/water): 75
Toxicity data: LD50 in mice, rats (g/kg): 1.3, 6.4 orally (Himmel)
Derivative Type: Dihydrochloride
CAS Registry Number: 57149-08-3
Molecular Formula: C24H28N2O3.2HCl
Molecular Weight: 465.41
Percent Composition: C 61.94%, H 6.50%, N 6.02%, O 10.31%, Cl 15.24%
Properties: Crystals from methanol/ethanol (1:2), mp 212-213°.
Melting point: mp 212-213°
Therap-Cat: Antihypertensive; a-blocker in treatment of symptomatic benign prostate hypertrophy.
Keywords: a-Adrenergic Blocker; Antihypertensive.

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