Naftopidil Inhibitor CAS No. 57149-07-2

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KI0768	Naftopidil	25 mg	$154
KI0768	Naftopidil	50 mg	$272

Chemical Characteristic

Product Name	Naftopidil
Synonyms	Flivas
CAS No.	57149-07-2
Molecular Weight	392.49
Formula	C₂₄H₂₈N₂O₃
Chemical Structure

Biological activities

Naftopidil is a selective α1-adrenergic receptor antagonist. The IC50 of naftopidil is 235 and 108 nM against α1-adrenoceptor and 5-HT1A receptor, respectively.[1] Naftopidil inhibits growths of androgen-sensitive and -insensitive human prostate cancer cell lines. Naftopidil prevents the growth of androgen-sensitive LNCaP cells and androgen-insensitive PC-3 cells with IC50 of 22.2 and 33.2 µM, respectively. In addition, naftopidil significantly increases expressions of p27kip1 and p21cip1 in PC-3 cells. In PC-3 cells, naftopidil induces p21cip1 but not p27kip1.[2] Naftopidil suppresses platelet aggregation with a Ki and a pIC50 of 1.1 µM and 5.09, respectively, with induction of aggregation 1 µM 5-HT. After oral administration of naftopidil, 5-HT-induced aggregation is significantly inhibited by 36%. Four hours after naftopidil administration, 5-HT uptake velocity is reduced by 33%.[3] Naftopidil reduces the growth of tumor in E9 cells (an androgen low-sensitive LNCaP subline). Naftopidil reveals antiproliferative effects on PCa cells regardless of androgen sensitivity and α1-AR subtype expression.[4] Intrathecal injection of naftopidil (3-30 µg) decreases the amplitude of bladder contraction.[5] Naftopidil significantly reduces Ki-67 index and increases the expression of p21cip1 in PC-3 tumors.[4]

Protocols

In vivo: Naftopidil is dissolved in 0.1 M phosphate solution.^[5]

References

[1] Borbe HO, et al. 5-HT1A-agonistic properties of naftopidil, a novel antihypertensive drug. Eur J Pharmacol. 1991, 205(1): 105-107. 閵嗏偓閵嗏偓 [2] Kanda H, et al. Naftopidil, a selective alpha-1 adrenoceptor antagonist, inhibits growth of human prostate cancer cells by G1 cell cycle arrest. Int J Cancer. 2008, 122(2): 444-451. 閵嗏偓閵嗏偓 [3] Kirsten R, et al. Naftopidil inhibits 5-hydroxytryptamine-induced platelet aggregation and 5-hydroxytryptamine uptake in platelets of healthy volunteers. Eur J Clin Pharmacol. 1994, 46(3): 271-274. 閵嗏偓閵嗏偓 [4] Hori Y, et al. Naftopidil, a selective α1-adrenoceptor antagonist, suppresses human prostate tumor growth by altering interactions between tumor cells and stroma. Cancer Prev Res (Phila). 2011, 4(1): 87-96. 閵嗏偓閵嗏偓 [5] Sugaya K, et al. Effects of intrathecal injection of tamsulosin and naftopidil, alpha-1A and -1D adrenergic receptor antagonists, on bladder activity in rats. Neurosci Lett. 2002, 328(1): 74-76. 閵嗏偓閵嗏偓

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