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Fig. 1 · Structure
Cat. No.
A10619
CAS No.
57149-08-3
Formula
C24H28N2O3.2HCl
Mol. Weight
465.4

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Naftopidil 2HCl

Cat. No. A10619 CAS 57149-08-3

5-HT1A and α1-adrenergic receptor antagonist

Naftopidil 2HCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.

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Biological Activity

Target & Activity

Target Activity Value
5-HT1A 0.1 μM
α1-adrenergic receptor 0.2 μM

In Vitro Studies

Naftopidil increased expression of the proapoptotic BH3-only proteins Bim, Puma and Noxa in SKOV3 and IGROV1-R10 cells. These changes were assessed by western blot and densitometry. In primary cultured rat USMCs, Naftopidil significantly reduced contraction activity. [1,2]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Proapoptotic Protein Expression in SKOV3 Cells

Cell-based study · SKOV3 [1]

SKOV3 cells received Naftopidil exposures of 25, 50 µM for a 48-h treatment. Western blot and densitometry showed increased expression of the proapoptotic BH3-only proteins Bim, Puma and Noxa.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
expression levels of BH3-only proteinsReported result Naftopidil (25, 50 µM), after a 48-h treatment: it increased that of the proapoptotic BH3-only Bim, Puma and Noxa proteins as depicted by western blot and densitometry quantification.[1]

Literature-Reported Treatment Conditions

Treatment concentration
25, 50 µM
Exposure duration
48-h treatment
Method
exposures
Vehicle
DMSO or ultra-pure water
Methods and source locations

Compound reported in the paper: Naftopidil

The paper names Naftopidil without stating the salt or form; not verified as the dihydrochloride form supplied as A10619. No dose conversion or lot validation.

Results > Naftopidil increases the expression of the proapoptotic Bim, Puma and Noxa proteins in a dose- and transcriptional-dependent manner (S7); Material and methods > Cell culture and treatment (S70); Fig. 1 legend (S124)

expression levels of BH3-only proteins: expression levels of BH3-only proteins; comparator: control conditions — Results > Naftopidil increases the expression of the proapoptotic Bim, Puma and Noxa proteins in a dose- and transcriptional-dependent manner (S7); Fig. 1 legend (S124)

Contraction Activity in Primary Rat USMCs

Cell-based study · primary cultured USMCs of rats [2]

Primary cultured rat USMCs were treated with Naftopidil at 86 ng/mL for 24 hours. Naftopidil significantly reduced contraction activity.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
positive pMLC areas in rat and human USMCsReported result Naftopidil; 86 ng/mL, for 24 hours: contraction activity was significantly reduced by naftopidil.[2]

Literature-Reported Treatment Conditions

Treatment concentration
86 ng/mL
Exposure duration
24 hours
Vehicle
methanol
Reported limits
Not stated in the sentences used: route.
Methods and source locations

Compound reported in the paper: Naftopidil

The paper names Naftopidil without stating the salt or form; not verified as the dihydrochloride form supplied as A10619. No dose conversion or lot validation.

MATERIALS AND METHODS > 4. Drugs and solutions (S24); MATERIALS AND METHODS > 6. Immunocytochemistry (S33, S36, S37); RESULTS > 2. In vitro relaxation induced by naftopidil (S56, S57, S59); Fig. 4 legend (S68, S69, S71, S72)

positive pMLC areas in rat and human USMCs: positive pMLC areas in rat and human USMCs; comparator: silodosin; 50 ng/mL, tamsulosin; 12 ng/mL — MATERIALS AND METHODS > 6. Immunocytochemistry (S33); RESULTS > 2. In vitro relaxation induced by naftopidil (S57); Fig. 4 legend (S68, S71)

Proapoptotic Protein Expression in IGROV1-R10 Cells

Cell-based study · IGROV1-R10 [1]

IGROV1-R10 cells received Naftopidil exposures of 25, 50 µM for a 48-h treatment. Western blot and densitometry showed increased expression of the proapoptotic BH3-only proteins Bim, Puma and Noxa.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
expression levels of BH3-only proteinsReported result Naftopidil (25, 50 µM), after a 48-h treatment: it increased that of the proapoptotic BH3-only Bim, Puma and Noxa proteins as depicted by western blot and densitometry quantification.[1]

Literature-Reported Treatment Conditions

Treatment concentration
25, 50 µM
Exposure duration
48-h treatment
Method
exposures
Vehicle
DMSO or ultra-pure water
Methods and source locations

Compound reported in the paper: Naftopidil

The paper names Naftopidil without stating the salt or form; not verified as the dihydrochloride form supplied as A10619. No dose conversion or lot validation.

Results > Naftopidil increases the expression of the proapoptotic Bim, Puma and Noxa proteins in a dose- and transcriptional-dependent manner (S7); Material and methods > Cell culture and treatment (S70); Fig. 1 legend (S124)

expression levels of BH3-only proteins: expression levels of BH3-only proteins; comparator: control conditions — Results > Naftopidil increases the expression of the proapoptotic Bim, Puma and Noxa proteins in a dose- and transcriptional-dependent manner (S7); Fig. 1 legend (S124)

In Vivo Studies

Oral Naftopidil was evaluated in wild-type mice with bleomycin-induced lung fibrosis. Concurrent Naftopidil treatment significantly reduced serum SP‐D levels compared with bleomycin administration alone. [3]

Serum SP‐D in Mice With Bleomycin-Induced Lung Fibrosis

Animal study · Wild‐type C57BL/6J mice; bleomycin‐induced lung fibrosis; BLM + naftopidil, n = 8 [3]

Wild-type mice with bleomycin-induced lung fibrosis received oral Naftopidil at 30 mg kg−1 d−1. Concurrent naftopidil treatment significantly reduced serum SP‐D levels compared with bleomycin administration alone.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
concentration of mouse serum SP‐D by enzyme‐linked immunosorbent assays 28 days after implanting the subcutaneous pumpReported result Naftopidil orally (30 mg kg−1 d−1), 5 days a week starting from 3 days before to 28 days after implanting the osmotic pump: concurrent naftopidil treatment significantly reduced serum SP‐D levels.[3]

Conditions shared by the study groups

Route
orally
Treatment course
5 days a week starting from 3 days before to 28 days after implanting the osmotic pump
Vehicle
0.1 mol/L citrate buffer (pH 4)
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Naftopidil 30 mg kg−1 d−1bleomycin administration (BLM, n = 7)Naftopidil orally (30 mg kg−1 d−1), 5 days a week starting from 3 days before to 28 days after implanting the osmotic pump: concurrent naftopidil treatment significantly reduced serum SP‐D levels.[3]
Naftopidil 30 mg kg−1 d−1
Model: Wild‐type C57BL/6J mice; bleomycin‐induced lung fibrosis; BLM + naftopidil, n = 8
Methods and source locations

Compound reported in the paper: Naftopidil

The paper names Naftopidil without stating the salt or form; not verified as the dihydrochloride form supplied as A10619. No dose conversion or lot validation.

MATERIALS AND METHODS > Animal procedures (S26, S27, S28); RESULTS > Effect of naftopidil on bleomycin‐induced lung fibrosis in mice (S68, S74, S75); Figure 5 legend (S117)

concentration of mouse serum SP‐D by enzyme‐linked immunosorbent assays 28 days after implanting the subcutaneous pump: concentration of mouse serum SP‐D by enzyme‐linked immunosorbent assays 28 days after implanting the subcutaneous pump; comparator: bleomycin administration (BLM, n = 7) — MATERIALS AND METHODS > Animal procedures (S28); RESULTS > Effect of naftopidil on bleomycin‐induced lung fibrosis in mice (S74, S75)

Naftopidil 30 mg kg−1 d−1 · MATERIALS AND METHODS > Animal procedures (S28); RESULTS > Effect of naftopidil on bleomycin‐induced lung fibrosis in mice (S75)

Specifications

Manufacturer Adooq Bioscience
Actions Antagonist
CAS Number 57149-08-3
Applications 5-HT1A and α1-adrenergic receptor antagonist
Formula C24H28N2O3.2HCl
Molecular Weight 465.4
Synonyms Flivas; KT-611; Avishot
SMILES
COC1=CC=CC=C1N2CCN(CC2)CC(COC3=CC=CC4=CC=CC=C43)O.Cl.Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 35 mg/mL (75.2 mM)
Water Insoluble
Ethanol 2 mg/mL (4.29 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
28 mg/mL
Vehicle
0.5% CMC

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Florent R, Weiswald LB, Lambert B, et al. Bim, Puma and Noxa upregulation by Naftopidil sensitizes ovarian cancer to the BH3-mimetic ABT-737 and the MEK inhibitor Trametinib. Cell Death Dis (2020). PMID: 32424251 DOI: 10.1038/s41419-020-2588-8 Source material
  2. [2] Hong SH, Jang EB, Hwang HJ, et al. Effect of α1D-adrenoceptor blocker for the reduction of ureteral contractions. Investig Clin Urol (2023). PMID: 36629069 DOI: 10.4111/icu.20220254 Source material
  3. [3] Urushiyama H, Terasaki Y, Nagasaka S, et al. Naftopidil reduced the proliferation of lung fibroblasts and bleomycin-induced lung fibrosis in mice. J Cell Mol Med (2019). PMID: 30873733 DOI: 10.1111/jcmm.14255 Source material

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