基本信息

技术规格

物性(参考值)

相关法规

基本信息

产品描述

Naftopidil 是选择性α1-肾上腺素能受体拮抗剂，或α受体抑制剂，Ki为58.3 nM。

靶点（IC50 & Targe）

α1A-adrenergic receptor,3.7nM(Ki)

α1B-adrenergic receptor,20nM(Ki)

α1D-adrenergic receptor,1.2nM(Ki)

体外研究

Naftopidil对alpha1d肾上腺素受体有比alpha1a和alpha1b肾上腺素受体亚型有更高的亲和力，分别达3倍和17倍。[1] 在雄激素敏感和不敏感的人前列腺癌细胞系中，Naftopidil有生长抑制效果。在PC-3细胞中，Naftopidil诱导p21基因（CIP1），但不是p27蛋白（kip1）。[2] 在所有检测的恶性间皮瘤细胞中，Naftopidil诱导凋亡，prazosin，一个α1肾上腺素受体阻断剂，产生类似的效果。Naftopidil诱导的细胞活力降低为GF109203X所抑制，而prazosin诱导的细胞活力影响较小。[3] Naftopidil，α1肾上腺素受体拮抗剂，产生浓度依赖性抑制胶原诱导的Ca2 +动员，40 mM Naftopidil导致最大抑制（22.9％）。Naftopidil也以浓度依赖的方式抑制肾上腺素诱导的Ca2+浓度上升（30 mM doxazosin），血小板聚集的抑制显著也正在生产。[4] Naftopidil（0.3，1和3 μM）浓度依赖性抑制5-HT诱导的膀胱收缩。Naftopidil同时抑制5-HT（2A）和5-HT（2）受体激动剂诱导的膀胱收缩。Naftopidil结合人5-HT（2A）和5-HT（2B）受体，pKi值分别为6.55和7.82。[5]

体内研究

与在麻醉狗模型平均血压相比，Naftopidil选择性地抑制phenylephrine诱导的前列腺的压力的增加。[1] 在大鼠中，Naftopidil通过阻断5-HT(2A)和5-HT(2B)受体来抑制5-HT诱导的膀胱收缩。[5]

参考文献

[1] Takei R, et al. Jpn J Pharmacol,?999, 79(4), 447-454.

[2] Kanda H, et al. Int J Cancer,?008, 122(2), 444-451.

[3] Masachika E, et al. Anticancer Res,?013, 33(3), 887-894.

[4] Alarayyed NA, et al. Br J Clin Pharmacol,?997, 43(4), 415-420.

[5] Sakai T, et al. Eur J Pharmacol,?013, 700(1-3), 194-200.

安全信息

图形或危害标志
提示语	Warning
危险说明	H302 H400 H410
防范说明	P264 P270 P273 P301 P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III
WGK	3
RTECS	TL9336500

产品说明

包装

25, 100 mg in poly bottle

生化/生理作用

α₁-Adrenoceptor antagonist; antihypertensive.

基本信息

产品性质

安全信息

基本信息

安全信息

图形或危害标志
危险性说明	H302: Harmful if swallowed. H315: Causes skin irritation. H319: Causes serious eye irritation. H335: May cause respiratory irritation. H361: Suspected of damaging fertility or the unborn child ..
防范说明	P201: Obtain special instructions before use. P202: Do not handle until all safety precautions have been read and understood. P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing P264: Wash hands thoroughly after handling. P270: Do not eat, drink or smoke when using this product. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P281: Use personal protective equipment as required. P301 + P312: IF SWALLOWED: Call a POISON CENTER or doctor/physician if you feel unwell. P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: . P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P308 + P313: IF exposed or concerned: Get medical advice/ attention. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see . on this label). P330: Rinse mouth. P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to local regulations.