产品说明书

Moxonidine

Print
Chemical Structure| 75438-57-2 同义名 : 莫索尼啶 ;BDF5895;LY326869
CAS号 : 75438-57-2
货号 : A482917
分子式 : C9H12ClN5O
纯度 : 98%
分子量 : 241.678
MDL号 : -
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(74.48 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Moxonidine is a selective agonist at the imidazoline receptor subtype 1 with very weak binding affinity for α2-adrenoceptors, used as antihypertensive agent[3]. Hypotensive and bradycardic actions of moxonidine but not clonidine are mediated through imidazoline receptors and are dependent on intact noradrenergic pathways within the RVLM(rostral ventrolateral medulla)[4]. Moxonidine binds with an affinity for the imidazoline I1 receptor that is 33 times more effective than is alpha2-receptor binding. There is a regression of left-ventricular hypertrophy after moxonidine was given for 6 months. Following oral administration the half-life (Tmax) is about 1 h. Moxonidine is highly bioavailable, approaching 90%[5]. Moreover, moxonidine (10 μmol·L-1) significantly inhibited the frequency of spontaneous EPSCs in both inspiratory-activated and inspiratory-inhibited AVPNs (airway vagal preganglionic neurons). Thus moxonidine inhibits the excitatory inputs to AVPNs via activation of both α2-adrenoceptors and imidazoline I1 receptors, and suggest that physiologically both of these two types of receptors are involved in the central regulation of airway vagal activity at preganglionic level[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02614794 HER2 Positive Breast Cancer Phase 2 Recruiting July 2021 -
NCT03622905 Alzheimer Disease Not Applicable Not yet recruiting October 1, 2024 -
NCT02574455 Breast Cancer Phase 3 Recruiting June 2020 -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.14mL

0.83mL

0.41mL

20.69mL

4.14mL

2.07mL

41.38mL

8.28mL

4.14mL
参考文献

[1]Alves TB, Totola LT, et al. GABA mechanisms of the nucleus of the solitary tract regulates the cardiovascular and sympathetic effects of moxonidine. Auton Neurosci. 2016 Jan;194:1-7.

[2]Gasparini S, Menani JV, et al. Moxonidine into the lateral parabrachial nucleus modifies postingestive signals involved in sodium intake control. Neuroscience. 2015 Jan 22;284:768-74.

[3]Schäfer U, Burgdorf C, Engelhardt A, Kurz T, Richardt G. Presynaptic effects of moxonidine in isolated buffer perfused rat hearts: role of imidazoline-1 receptors and alpha2-adrenoceptors. J Pharmacol Exp Ther. 2002 Dec;303(3):1163-70

[4]Chan CK, Burke SL, Zhu H, Piletz JE, Head GA. Imidazoline receptors associated with noradrenergic terminals in the rostral ventrolateral medulla mediate the hypotensive responses of moxonidine but not clonidine. Neuroscience. 2005;132(4):991-1007

[5]Prichard BN, Graham BR, Owens CW. Moxonidine: a new antiadrenergic antihypertensive agent. J Hypertens Suppl. 1999 Aug;17(3):S41-54

[6]Zhou X, He D, Yan X, Chen X, Li R, Zhang G, Wang J. Moxonidine inhibits excitatory inputs to airway vagal preganglionic neurons via activation of both α2-adrenoceptors and imidazoline I1 receptors. Brain Res. 2020 Apr 1;1732:146695