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吡那地尔

吡那地尔用途

【用途一】
钾通道开放剂，通过开放平滑肌细胞中钾通道，使钾流出和静息膜电位负偏移，静止时细胞超极化，导致细胞内钙离子减少，平滑肌松弛，尤其是脉管系统平滑肌松弛。用于高血压。

吡那地尔名称

[ CAS 号 ]:
85371-64-8

[ 中文名 ]:
吡那地尔

[ 英文名 ]:
Pinacidil hydrate

[中文别名 ]:

[英文别名 ]:

Pinacidil (hydrate)
Pinacidil . monohydrate
MFCD00242745
Hndac
Pinacidil monohydrate
EINECS 262-294-9
Pinacidil hydrate

吡那地尔生物活性

[ 描述 ]:

Pinacidil monohydrate,一种抗高血压药,是一种钾通道激活剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钾通道

研究领域 >> 其他

[体外研究]

吡那地尔一水合物是钾通道活化剂[1]。吡那地尔水合物是一种称为“钾通道开放剂”的一类抗高血压药物[2]。吡那地尔水合物激活豚鼠膀胱和心脏的ATP调节钾通道,Ki值分别为104和251 nM [3]。

[参考文献]

[1]. Buckle DR, et al. Relaxant effects of the potassium channel activators BRL 38227 and pinacidil on guinea-pig and human airway smooth muscle, and blockade of their effects by glibenclamide and BRL 31660. Pulm Pharmacol. 1993 Mar;6(1):77-86.

[2]. Bareggi SR, et al. Pharmacodynamics and pharmacokinetics of pinacidil in normotensive volunteers after repeated doses of a new slow-release tablet formulation. Arzneimittelforschung. 1999 Jan;49(1):21-5.

[3]. Gollasch M, et al. Pinacidil relaxes porcine and human coronary arteries by activating ATP-dependent potassium channels in smooth muscle cells. J Pharmacol Exp Ther. 1995 Nov;275(2):681-92.

[相关活性小分子]

吡那地尔物理化学性质

[ 沸点 ]:
356.7ºC at 760 mmHg

[ 熔点 ]:
164-165ºC

[ 分子式 ]:
C₁₃H₂₁N₅O

[ 分子量 ]:
263.34

[ 闪点 ]:
169.5ºC

[ PSA ]:
73.10000

[ LogP ]:
2.94578

[ 外观性状 ]:
粉末

[ 储存条件 ]:
2-8℃

[ 水溶解性 ]:
ethanol: 14 mg/mL

吡那地尔MSDS

详细MSDS(安全技术说明书)

吡那地尔安全信息

[ 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) ]:
S36

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

[ WGK德国 ]:
3

[ 海关编码 ]:
2933399090

吡那地尔制备

【方法一】
方法1：化合物(I)溶于四氢呋喃，在0℃加入光气的甲苯溶液，反应5h。蒸出溶剂后，加入乙基二异丙基胺处理，得化合物(Ⅱ)。再和氰胺反应，得吡那地尔。
方法2：氰胺和乙基二异丙基胺反应后，再加入4-吡啶基异氰酸酯反应，得化合物(Ⅲ)。甲基化得(Ⅳ)，再和胺反应得吡那地尔。

吡那地尔海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 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 ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

吡那地尔文献

Evidence against a systemic arterial defect in patients with inflammatory bowel disease.

J. Surg. Res. 191(2) , 318-22, (2014)

Despite increasing interest in local microvascular alterations associated with inflammatory bowel disease (IBD), the potential contribution of a primary systemic vascular defect in the etiology of IBD...

Kcnh2 and Kcnj8 interactively regulate skin wound healing and regeneration.

Wound Repair Regen. 23 , 797-806, (2015)

Previous studies indicate that ion channels are mediators of bioelectricity promoting wound closure/regeneration in nonmammalian, lower vertebrate systems. The role of ion channels however in regenera...

Potassium ion channels and allergic asthma.

Adv. Exp. Med. Biol. 838 , 35-45, (2015)

High-conductive calcium-sensitive potassium channels (BK+Ca) and ATP-sensitive potassium (K+ATP) channels play a significant role in the airway smooth muscle cell and goblet cell function, and cytokin...

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