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莫索尼定

莫索尼定

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?莫索尼定名称


















中文名

莫索尼啶
英文名

4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine
中文别名


莫索尼定,不带盐酸




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4-氯-N-(4,5-二氢-1H-咪唑-2-基)-6-甲氧基-2-甲基-5-嘧啶胺




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莫索尼定



英文别名
更多





?莫索尼定生物活性












































描述
Moxonidine(BDF5895)是咪唑啉1型受体(I1-R)选择性激动剂,为降压剂。
相关类别




溶解度

体外:

在DMSO中10mM


储备液

1 mM 4.1377 mL 20.6885 mL 41.3770 mL
5 mM 0.8275 mL 4.1377 mL 8.2754 mL
10 mM 0.4138 mL 2.0689 mL 4.1377 mL


存储

粉末 -20°C 3年
? 4°C 2年
在溶剂中 -80°C 6月
? -20°C 1月


运输

室温;可能会有所不同
SMILES

CC1=NC(OC)=C(NC2=NCCN2)C(Cl)=N1
参考文献

[1]. Schafer, U., et al., Presynaptic effects of moxonidine in isolated buffer perfused rat hearts: role of imidazoline-1 receptors and alpha2-adrenoceptors. J Pharmacol Exp Ther, 2002. 303(3): p. 1163-70.

[2]. Chan, C.K., et al., Imidazoline receptors associated with noradrenergic terminals in the rostral ventrolateral medulla mediate the hypotensive responses of moxonidine but not clonidine. Neuroscience, 2005. 132(4): p. 991-1007.


相关活性
小分子




1-(4-氨丁基)胍硫酸盐



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尿囊素



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盐酸莫索尼定



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CR4056






?莫索尼定物理化学性质

















































密度 1.5±0.1 g/cm3
沸点 364.7±52.0 °C at 760 mmHg
熔点 40-43?°C(lit.)
分子式 C9H12ClN5O
分子量 241.678
闪点 174.3±30.7 °C
精确质量 241.073044
PSA 71.43000
LogP 0.84
外观性状 晶体
蒸汽压 0.0±0.8 mmHg at 25°C
折射率 1.681
储存条件 Desiccate at +4°C
计算化学

1.疏水参数计算参考值(XlogP):0.6

2.氢键供体数量:2

3.氢键受体数量:4

4.可旋转化学键数量:3

5.互变异构体数量:2

6.拓扑分子极性表面积71.4

7.重原子数量:16

8.表面电荷:0

9.复杂度:275

10.同位素原子数量:0

11.确定原子立构中心数量:0

12.不确定原子立构中心数量:0

13.确定化学键立构中心数量:0

14.不确定化学键立构中心数量:0

15.共价键单元数量:1

更多

1.性状:结晶

2.熔点(?C):217-219℃(分解)。






?莫索尼定安全信息




















危险品运输编码 NONH for all modes of transport
WGK德国 3
RTECS号 UV6260290





?莫索尼定合成线路
















?莫索尼定制备


方法1:5-氨基-4,6-二氯-2-甲基嘧啶和1-乙酰基-2-咪唑啉-2-酮反应,生成的产物和甲醇钠作用得莫索尼定。

75438-57-2 preparation
方法2:5-氨基-4-氯-6-甲氧基-2-甲基嘧啶和硫氰酸铵及苯甲酰氯反应,得(I)。去苯甲酰基得(Ⅱ),甲基化得(Ⅲ),再和乙二胺作用得莫索尼定。

75438-57-2 preparation










?莫索尼定文献42

更多文献














Selective imidazoline agonist moxonidine plus the ACE inhibitor ramipril in hypertensive patients with impaired insulin sensitivity: partners in a successful MARRIAGE?

Curr. Med. Res. Opin. 20(3) , 359-67, (2004)

Hypertension in combination with clinically overt diabetes mellitus is recognized as a particularly powerful combination of risk factors that greatly increases cardiovascular vulnerability. There is a...





Moxonidine: a review of safety and tolerability after seven years of clinical experience.

J. Hypertens. 17 , S37-S39, (1999)

Centrally acting antihypertensive drugs, or sympatholytics, (reserpine, methyldopa and clonidine) have a long history of efficacy but are now little used in most countries. One of the most important r...





[The efficacy of antihypertension drugs and their combinations in the non-treated hypertension].

Med. Tr. Prom. Ekol. (5) , 7-11, (2013)

In case of non-treated hypertension several medications and their combinations were studied (captopril, and moxonidine as such, captopril + nifedipine, captopril + moxonidine). Moxonidine to be more e…









?莫索尼定英文别名








































































4-chloro-5-(imidazoline-2-ylamino)-6-methoxy-2-methylpyrimidine


[3H]-Moxonidine


4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine


4-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methyl-5-pyrimidinamine


Norcynt


4-Chloro-N-(imidazolidin-2-ylidene)-6-methoxy-2-methylpyrimidin-5-amine


BE 5895


5-Pyrimidinamine, 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methyl-


Normoxocin


Lomox


4-chloro-N-(4,5-dihydro-1H9imidazol-yl)-6-methoxy-2-methyl-5-pyrimidinamine


Physiotens


[14C]-Moxonidine


4-chloro-5-[(4,5-dihydro-1H-imidazol-2-yl)-amino]-6-methoxy-2-methylpyrimidine


T6N CNJ B1 DO1 FG EM- BT5M CN BUTJ


Nucynt


Cynt


Moxonidinum [Latin]


Moxonidine


T6N CNJ B1 DO1 FG ENU- BT5MYMTJ


MFCD06795643








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