Naftopidil is a selective α1-adrenergic receptor antagonist or α receptor inhibitor with Ki of 58.3 nM. In vivo, forty minutes after the intravenous administration of naftopidil, the selectivity index was 3.76, naftopidil selectively inhibited the phenylephrine-induced increase in prostatic pressure[3]. In vitro, the concentrations causing 50% inhibition (IC50) of cancer cell growth were 22.2 ± 4.0 microM in androgen-sensitive LNCaP cells and 33.2 ± 1.1 microM in androgen-insensitive PC-3 cells. In vivo, oral administration of naftopidil to nude mice inhibited the growth of PC-3 tumors as compared to vehicle-treated controls[4]. Moreover, naftopidil induced apoptosis in all the investigated malignant mesothelioma cells[5].
Naftopidil/萘哌地尔 细胞实验
Cell Line
Concentration
Treated Time
Description
References
IGROV1-R10 cells
50 µM
48 h
Naftopidil inhibited IGROV1-R10 cell proliferation and increased the expression of BH3-only proteins Bim, Puma, and Noxa
Cell Death Dis. 2020 May 18;11(5):380.
SKOV3 cells
50 µM
48 h
Naftopidil inhibited SKOV3 cell proliferation and increased the expression of BH3-only proteins Bim, Puma, and Noxa
Cell Death Dis. 2020 May 18;11(5):380.
LL97A
0-80 µmol/L
48 h
Naftopidil decreased the proliferation of LL97A cells in a dose-dependent manner
J Cell Mol Med. 2019 May;23(5):3563-3571.
TIG-1-20
0-80 µmol/L
48 h
Naftopidil decreased the proliferation of TIG-1-20 cells in a dose-dependent manner
J Cell Mol Med. 2019 May;23(5):3563-3571.
WI-38
0-80 µmol/L
48 h
Naftopidil decreased the proliferation of WI-38 cells in a dose-dependent manner
J Cell Mol Med. 2019 May;23(5):3563-3571.
KGN cells
20 µM
24 h
To verify the regulatory effects of (R)-NAF and (S)-NAF on UGT2B15 expression, results showed they upregulated UGT2B15 expression and reduced DHT accumulation.
J Ovarian Res. 2025 Jan 24;18(1):13.
Naftopidil/萘哌地尔 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
Bleomycin-induced lung fibrosis model
Oral
30 mg/kg
5 days a week for 28 days
Naftopidil attenuated bleomycin-induced lung fibrosis, reduced collagen deposition and the number of α-SMA-positive myofibroblasts, and decreased serum surfactant protein-D levels
J Cell Mol Med. 2019 May;23(5):3563-3571.
C57BL/6J mice
PCOS mouse model
Oral gavage
10 mg/mL
Once daily for 6 weeks
To evaluate the ameliorative effects of (R)-NAF and (S)-NAF on PCOS symptoms in mice, results showed they upregulated UGT2Bs expression, reduced androgen accumulation, and improved ovarian morphology and menstrual cycles.
Brazil
... 展开 >> Hospital das Clínicas da Faculdade de Medicina da USP
Not yet recruiting
São Paulo, Brazil, 05403-010
Contact: Geraldo C Freire, PhD 55 11 3069-8082
Contact: Camila C Marin 55 11 3069-8082 camila.marin@ig.com.br
Principal Investigator: Geraldo C Freire, PhD 收起 <<
Brazil
... 展开 >> Hospital das Clínicas da Faculdade de Medicina da USP
Not yet recruiting
São Paulo, Brazil, 05403-010
Contact: Geraldo C Freire, PhD 55 11 3069-8082
Contact: Camila C Marin 55 11 3069-8082 camila.marin@ig.com.br
Principal Investigator: Geraldo C Freire, PhD 收起 <<
Korea, Republic of
... 展开 >>
Seoul National University Bundang Hospital
Seongnam, Kyunggi, Korea, Republic of, 463-712
Kangwon National University Hospital
Chuncheon, Korea, Republic of
Donguk University Ilsan Hospital
Goyang, Korea, Republic of
Seoul National University Hospital
Seoul, Korea, Republic of, 110-744
National Medical Center
Seoul, Korea, Republic of
Seoul National University Boramae Hospital
Seoul, Korea, Republic of 收起 <<
Korea, Republic of
... 展开 >>
Donguk University Ilsan Hospital
Goyang, Kyunggi, Korea, Republic of
Seoul National University Bundang Hospital
Seongnam, Kyunggi, Korea, Republic of, 463-712
Kangwon National University Hospital
Chuncheon, Korea, Republic of
Seoul National University Hospital
Seoul, Korea, Republic of, 110-744
National Medical Center
Seoul, Korea, Republic of
Seoul National University Boramae Medical Center
Seoul, Korea, Republic of 收起 <<
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