米诺地尔硫酸盐

米诺地尔硫酸盐用途

Minoxidil sulfate 是一种有效的 ATP 敏感的 K+ 通道 (K+ channel) 激动剂,是米诺地尔的硫酸代谢物。Minoxidil sulfate 被认为是一种血管扩张试剂,在动物实验模型中,促进头发生长。

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米诺地尔硫酸盐作用

1.舒缓扩张心血管药：本品为钾离子通道开放剂，能直接松弛血管平滑肌，有强大的小动脉扩张作用，使外周阻力下降，血压下降，而对容量血管无影响，故能促进静脉回流。
2.降血压药：反射性调节作用和正性频率作用，可使心输出量及心率增加，但不引起体位性低血压。

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米诺地尔硫酸盐名称

[ CAS 号 ]:
83701-22-8

[ 中文名 ]:
敏乐啶硫酸盐

[ 英文名 ]:
Minoxidil sulphate

[中文别名 ]:

[英文别名 ]:

MFCD06248907
Minoxidil sulphate

米诺地尔硫酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 代谢疾病

信号通路 >> 跨膜转运 >> 钾通道

[ 靶点 ]

IC50: K channel[2]

[体外研究]

硫酸米诺地尔(1-100μM；2小时)以时间依赖性的方式显著降低RBMEC单层中血脑肿瘤屏障(BTB)的通透性,另外,MS对跨内皮电阻(TEER)的影响是高浓度2小时的跨内皮电阻(TEER)[2]。硫酸米诺地尔(0-100μM；0-4h)可使脑肿瘤组织RhoA活性增加1h,最高水平出现在2h,并显著诱导ser473处短暂的PKB磷酸化,而不影响PKB的总水平。另外,LY294002部分阻止了MS诱导的PKB磷酸化[2]。Western Blot分析[2]细胞系：大鼠脑微血管内皮细胞(RBMECs)浓度：0-100μM孵育时间：15min、30min、1h、2h、4h。结果：诱导RhoA激活和ser473处PKB磷酸化。

[参考文献]

[1]. A E Buhl, et al. Minoxidil sulfate is the active metabolite that stimulates hair follicles. J Invest Dermatol. 1990 Nov;95(5):553-7.

[2]. Yan-ting Gu, et al. Minoxidil sulfate induced the increase in blood-brain tumor barrier permeability through ROS/RhoA/PI3K/PKB signaling pathway.Neuropharmacology 2013 Dec;75:407-15.doi: 10.1016/j.neuropharm.

[3]. Y Nakaya, et al.Effect of minoxidil sulfate and pinacidil on single potassium channel current in cultured human outer root sheath cells and dermal papilla cells. J Dermatol Sci. 1994 Jul;7 Suppl:S104-8.

米诺地尔硫酸盐物理化学性质

[ 沸点 ]:
732ºC at 760 mmHg

[ 熔点 ]:
175-180°C

[ 分子式 ]:
C₉H₁₅N₅O₄S

[ 分子量 ]:
289.311

[ 闪点 ]:
396.5ºC

[ 精确质量 ]:
289.084473

[ PSA ]:
146.86000

[ LogP ]:
0.72080

[ 外观性状 ]:
白色结晶固体

[ 储存条件 ]:
−20°C

[ 稳定性 ]:
Light Sensitive - Protect from Light, Store in Freezer

米诺地尔硫酸盐安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ 海关编码 ]:
2933599090

米诺地尔硫酸盐海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

米诺地尔硫酸盐文献

Molecular biology of the human cytosolic sulfotransferase gene superfamily implicated in the bioactivation of minoxidil and cholesterol in skin.

Exp. Dermatol. 8(4) , 328-9, (1999)

Cytosolic sulfotransferases (ST) catalyze the sulfation of various phenolic agents, catecholamines, thyroid hormones, steroids, drugs, and procarcinogens, usually resulting in the inactivation and sub...

Iontophoresis-targeted, follicular delivery of minoxidil sulfate for the treatment of alopecia.

J. Pharm. Sci. 102(5) , 1488-94, (2013)

Although minoxidil (MX) is a drug known to stimulate hair growth, the treatment of androgenic alopecia could be improved by delivery strategies that would favor drug accumulation into the hair follicl...

Sulfation of minoxidil by multiple human cytosolic sulfotransferases.

Chem. Biol. Interact. 109(1-3) , 53-67, (1998)

Minoxidil is an antihypertensive agent and hair growth promoter that is metabolized by sulfation to the active compound, minoxidil sulfate. Thermostable phenol sulfotransferase (TS PST or P-PST) was i...

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