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莫索尼定

莫索尼定用途

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

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莫索尼定名称

[ CAS 号 ]:
75438-57-2

[ 中文名 ]:
莫索尼啶

[ 英文名 ]:
Moxonidine

[中文别名 ]:

[英文别名 ]:

[3H]-Moxonidine
Norcynt
BE 5895
Normoxocin
Lomox
Physiotens
[14C]-Moxonidine
T6N CNJ B1 DO1 FG EM- BT5M CN BUTJ
Nucynt
Cynt

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 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 咪唑啉受体

信号通路 >> 神经信号通路 >> 咪唑啉受体

研究领域 >> 神经疾病

[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]

硫酸胍基丁胺 | 尿囊素 | 盐酸莫索尼定 | 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

莫索尼定安全信息

[ 危害码 (欧洲) ]:
Xn

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UV6260290

[ 危险类别 ]:
6.1

莫索尼定合成路线

详细合成路线

莫索尼定上下游产品

莫索尼定上游产品

莫索尼定下游产品

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。

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。

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莫索尼定文献

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...

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