Fabomotizole hydrochloride (CM346 hydrochloride)
(Synonyms: CM346 hydrochloride) 目录号 : GC30903
A multi-targeted anxiolytic drug with neuroprotective activities
Cas No.:173352-39-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Afobazole is a multi-targeted anxiolytic drug with neuroprotective activities.1,2 It binds to the sigma-1, melatonin MT1, and MT3 receptors, as well as monoamine oxidase A (MAO-A; Kis = 5.9, 160, 0.97, and 3.6 ?M, respectively, in a radioligand binding assay).1 Afobazole (5 mg/kg) decreases the latency to enter, as well as increases the number of entries into and percentage of time spent in, the open arms of the elevated plus maze, indicating anxiolytic-like activity in passive stress-coping BALB/c, but not active stress-coping C57BL/6, mice.3 It decreases stroke volume and neuronal and oligodendroglial cell death in the brain in a rat model of ischemia induced by middle cerebral artery occlusion (MCAO) when administered at doses of 0.3 and 3 mg/kg.2
1.Seredenin, S.B., and Voronin, M.V.[Neuroreceptor mechanisms of the afobazole effect]Eksp. Klin. Farmakol.72(1)3-11(2009) 2.Katnik, C., Garcia, A., Behensky, A.A., et al.Treatment with afobazole at delayed time points following ischemic stroke improves long-term functional and histological outcomesNeurobiol. Dis.62354-364(2014) 3.Anderzhanova, E.A., B?chli, H., Buneeva, O.A., et al.Strain differences in profiles of dopaminergic neurotransmission in the prefrontal cortex of the BALB/C vs. C57Bl/6 mice: Consequences of stress and afobazoleEur. J. Pharmacol.708(1-3)95-104(2013)
| Cas No. | 173352-39-1 | SDF | |
| 别名 | CM346 hydrochloride | ||
| Canonical SMILES | CCOC1=CC=C2C(N=C(SCCN3CCOCC3)N2)=C1.Cl | ||
| 分子式 | C15H22ClN3O2S | 分子量 | 343.87 |
| 溶解度 | DMSO : ≥ 44 mg/mL (127.96 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9081 mL | 14.5404 mL | 29.0808 mL |
| 5 mM | 0.5816 mL | 2.9081 mL | 5.8162 mL |
| 10 mM | 0.2908 mL | 1.454 mL | 2.9081 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Anti-Ischemic Activity of Fabomotizole Hydrochloride under Conditions of Endothelial Dysfunction
Anti-ischemic activity of fabomotizole hydrochloride was studied on the model of subendocardial ischemia in rats with endothelial dysfunction. Endothelial dysfunction was modeled by intragastric administration of methionine (3 g/kg, once a day for 7 days). Acute subendocardial ischemia was induced in narcotized rats by intraperitoneal injection of isoproterenol (20 μg/kg/min over 5 min). Fabomotizole hydrochloride (intraperitoneally, 15 mg/kg) significantly reduced isoproterenol-induced ST segment depression in animals with endothelial dysfunction and with intact vasculature.
Examination of Cardioprotective Effects of Fabomotizole Hydrochloride in Translational Rat Model of Chronic Heart Failure
A translational rat model of chronic heart failure was employed to examine the cardioprotective effect of fabomotizole hydrochloride. Fabomotizole therapy for 28 days (15 mg/kg/day intraperitoneally) restored inotropic function of the left ventricle and increased ejection fraction from 54±3 to 65±3% (p=0.001). The inotropic function returned to normal against the background of significantly reduced myocardial expression of angiotensin (p=0.01) and glucocorticoid (p=0.03) receptors and significant increased expression of sigma-1 receptors (p=0.04). Inhibition of abnormal expression of angiotensin and glucocorticoid receptors responsible for activation of the pathological cascades underlying the postinfarction remodeling of the left ventricle as well as activation of the expression of cytoprotective sigma-1 receptors are viewed as the key features of the cardioprotective action of fabomotizole hydrochloride.
On the Mechanism of the Cardioprotective Action of σ1 Receptor Agonist Anxiolytic Fabomotizole Hydrochloride (Afobazole)
Original translational rat model of chronic heart failure provoked by experimental anterior transmural myocardium infarction was employed to examine the preventive action of anxiolytic Afobazole (15 mg/kg/day administered intraperitoneally during the first 15 days after coronary occlusion) on the development of the heart failure assessed in 3 months after infarction. Afobazole prevented the development of pathologic remodeling of the myocardium, maintained its inotropic function, and decreased the plasma level of brain natriuretic peptide known as a biochemical marker of chronic heart failure. In the myocardium, Afobazole down-regulated overexpression of the genes induced in chronic heart failure and assessed by corresponding RNA levels, which code angiotensin (AT1A-R), vasopressin (V1A-R), and glucocorticoid (GR) receptors as well as Epac2 protein. The revealed biochemical changes are consistent with the data on cardioprotective action of Afobazole.