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57149-07-2

57149-07-2 structure
57149-07-2 structure
  • Name: Naftopidil
  • Chemical Name: Naftopidil dihydrochloride
  • CAS Number: 57149-07-2
  • Molecular Formula: C24H28N2O3
  • Molecular Weight: 392.491
  • Catalog: API Circulatory system medication Prevention and treatment of angina pectoris
  • Create Date: 2018-03-09 08:00:00
  • Modify Date: 2025-08-20 15:02:13
  • Naftopidil (Flivas), a selective α1-adrenergic receptor antagonist or alpha blocker, is an antihypertensive drug.Target: α1-Adrenergic ReceptorNaftopidil significantly improved the overall international prostatic symptom score ; from 19.2±7.9 to 11.7±5.8 in the M group and from 19.4±6.4 to 12.3±6.8 in the E group (p<0.0001), QOL score from 4.9±0.8 to 3.2±1.4 in the M group and from 5.0±0.8 to 3.6±1.3 in the E group (p<0.0001), and OAB symptom score from 7.8±2.6 to 5.0±2.5 in the M group (p<0.0001) and from 8.6±2.9 to 5.8± 3.3 in the E group (p<0.0001). naftopidil improves storage symptoms as well as voiding symptoms regardless of timing of administration [1]. The selectivity of naftopidil for prostatic pressure was the most potent among the test compounds. In addition, using cloned human alpha1-adrenoceptor subtypes, naftopidil was selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. The selectivity of naftopidil for prostatic pressure may be attributable to its high binding affinity for alpha1a- and alpha1d-adrenoceptor subtypes [2].

Name Naftopidil dihydrochloride
Synonyms Avishot
Naftopiil
Naftopidildihydrochloride
RS-1-[4-(2-Methoxyphenyl)-1-piperazinyl]-3-(1-naphthoxy)-2-propanol
1-(2-Methoxyphenyl)-4-[3-(naphth-1-yloxy)-2-hydroxypropyl]-piperazine
4-(2-Methoxyphenyl)-a-[(1-naphthalenyloxy)methyl]-1-piperazineethanol
NafTopIDi1
Flivas
1-[4-(2-Methoxyphenyl)-1-piperazinyl]-3-(1-naphthyloxy)-2-propanol
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-(naphthalen-1-yloxy)propan-2-ol
Naftopil
Naftopidil and intermediates
MFCD00242741
kt-611
1-Piperazineethanol, 4-(2-methoxyphenyl)-α-[(1-naphthalenyloxy)methyl]-
Naftopidil
1-[4-(2-Methoxyphenyl)piperazin-1-yl]-3-(1-naphthyloxy)propan-2-ol
Description Naftopidil (Flivas), a selective α1-adrenergic receptor antagonist or alpha blocker, is an antihypertensive drug.Target: α1-Adrenergic ReceptorNaftopidil significantly improved the overall international prostatic symptom score ; from 19.2±7.9 to 11.7±5.8 in the M group and from 19.4±6.4 to 12.3±6.8 in the E group (p<0.0001), QOL score from 4.9±0.8 to 3.2±1.4 in the M group and from 5.0±0.8 to 3.6±1.3 in the E group (p<0.0001), and OAB symptom score from 7.8±2.6 to 5.0±2.5 in the M group (p<0.0001) and from 8.6±2.9 to 5.8± 3.3 in the E group (p<0.0001). naftopidil improves storage symptoms as well as voiding symptoms regardless of timing of administration [1]. The selectivity of naftopidil for prostatic pressure was the most potent among the test compounds. In addition, using cloned human alpha1-adrenoceptor subtypes, naftopidil was selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. The selectivity of naftopidil for prostatic pressure may be attributable to its high binding affinity for alpha1a- and alpha1d-adrenoceptor subtypes [2].
Related Catalog
References

[1]. Sakai, H., et al., [Efficacy of naftopidil in patients with overactive bladder associated with benign prostatic hyperplasia: prospective randomized controlled study to compare differences in efficacy between morning and evening medication]. Hinyokika Kiyo

[2]. Takei, R., et al., Naftopidil, a novel alpha1-adrenoceptor antagonist, displays selective inhibition of canine prostatic pressure and high affinity binding to cloned human alpha1-adrenoceptors. Jpn J Pharmacol, 1999. 79(4): p. 447-54.

Density 1.2±0.1 g/cm3
Boiling Point 602.8±55.0 °C at 760 mmHg
Melting Point 127 °C
Molecular Formula C24H28N2O3
Molecular Weight 392.491
Flash Point 318.3±31.5 °C
Exact Mass 392.209991
PSA 45.17000
LogP 4.81
Vapour Pressure 0.0±1.8 mmHg at 25°C
Index of Refraction 1.619
Storage condition Store at RT
Water Solubility methanol: >10 mg/mL

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TL9336500
CHEMICAL NAME :
1-Pioerazineethanol, 4-(2-methoxyphenyl)-alpha-((1-naphthalenyloxy)methyl) -
CAS REGISTRY NUMBER :
57149-07-2
BEILSTEIN REFERENCE NO. :
0629965
LAST UPDATED :
199806
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C24-H28-N2-O3
MOLECULAR WEIGHT :
392.54

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
4320 mg/kg
SEX/DURATION :
female 16 day(s) after conception - 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 48,7,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1080 mg/kg
SEX/DURATION :
female 16 day(s) after conception - 21 day(s) post-birth
TOXIC EFFECTS :
Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 48,7,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
15680 mg/kg
SEX/DURATION :
male 9 week(s) pre-mating female 2 week(s) pre-mating - 3 week(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 48,17,1994
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
1300 mg/kg
SEX/DURATION :
female 7-19 day(s) after conception
TOXIC EFFECTS :
Reproductive - Maternal Effects - other effects Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 48,1,1994
Hazard Codes Xi
WGK Germany 3
RTECS TL9336500
HS Code 2942000000
HS Code 2942000000
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