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    InvivoChem Cat #: V1113
    CAS #: 57149-07-2Purity ≥98%

    Description: Naftopidil (BM-15275; KT611; BM15275; KT611; Flivas) is a selective α1-adrenergic receptor antagonist that has been approved for the treatment of BPH-benign prostatic hyperplasia. Naftopidil inhibits α1a, α1b, and α1d-adrenoceptors with Kis of 3.7 nM, 20 nM, and 1.2 nM, respectively.

    References: Jpn J Pharmacol. 1999 Apr;79(4):447-54; Eur J Pharmacol. 2013 Jan 30;700(1-3):194-200. 

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    Molecular Weight (MW)392.49 
    CAS No.57149-07-2 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 79 mg/mL (201.3 mM) 
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Chemical Name1-(4-(2-methoxyphenyl)piperazin-1-yl)-3-(naphthalen-1-yloxy)propan-2-ol diHCl
    SynonymsKT-611; BM-15275; KT611; BM 15275; KT 611; BM15275; KT611; Flivas 

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    In Vitro

    In vitro activity: Naftopidil is selective for the alpha1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the alpha1a- and alpha1b-adrenoceptor subtypes, respectively. Naftopidil has growth inhibitory effect in androgen-sensitive and -insensitive human prostate cancer cell lines. Naftopidil induces p21(cip1) but not p27(kip1) in PC-3 cells. Naftopidil induces apoptosis in all the investigated malignant mesothelioma cells, and a similar effect is obtained with prazosin, another α1-adrenoceptor blocker. Naftopidil-induced reduction in cell viability is inhibited by GF109203X, while prazosin-induced in cell viability is less affected. Naftopidil, an alpha 1-adrenoreceptor antagonist produces a concentration-dependent inhibition ofcollagen-induced Ca2+ mobilization, maximum inhibition (22.9%) occurring with 40 mM Naftopidil. Naftopidil also inhibits the adrenaline-induced rise in [Ca2+]i in a concentration-dependent manner (30 mM doxazosin), significant inhibitions of platelet aggregation also being produced. Naftopidil (0.3, 1, and 3 μM) inhibits 5-HT-induced bladder contraction in a concentration-dependent manner. Naftopidil inhibits both the 5-HT(2A) and 5-HT(2) receptor agonists-induced bladder contractions. Naftopidil binds to the human 5-HT(2A) and 5-HT(2B) receptors with pKi values of 6.55 and 7.82, respectively.

    In VivoNaftopidil selectively inhibits the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. Naftopidil inhibits 5-HT-induced bladder contraction via blockade of the 5-HT(2A) and 5-HT(2B) receptors in rats.  
    Animal modelRats and dogs
    Formulation & DosageN/A

    Jpn J Pharmacol. 1999 Apr;79(4):447-54; Eur J Pharmacol. 2013 Jan 30;700(1-3):194-200.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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