For research use only.
Catalog No.S2126 Synonyms: KT-611
CAS No. 57149-07-2
Naftopidil (KT-611) is a selective α1-adrenergic receptor antagonist with Ki of 3.7 nM, 20 nM, and 1.2 nM for α1a, α1b, and α1d, respectively, used for the treatment of benign prostatic hyperplasia.
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|Description||Naftopidil (KT-611) is a selective α1-adrenergic receptor antagonist with Ki of 3.7 nM, 20 nM, and 1.2 nM for α1a, α1b, and α1d, respectively, used for the treatment of benign prostatic hyperplasia.|
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 vivo||Naftopidil 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. |
-  Takei R, et al. Jpn J Pharmacol,?999, 79(4), 447-454.
-  Kanda H, et al. Int J Cancer,?008, 122(2), 444-451.
-  Masachika E, et al. Anticancer Res,?013, 33(3), 887-894.
|In vitro||DMSO||79 mg/mL (201.27 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00967772||Completed||Drug: Naftopidil||Healthy||Dong-A ST Co. Ltd.||September 2009||Phase 1|
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