Amezinium methylsulfate (Amezinium metilsulfate)
(Synonyms: 甲磺美嗪,Amezinium metilsulfate; Lu-1631) 目录号 : GC32516
Amezinium is a sympathomimetic used for its vasopressor effects in the treatment of hypotensive states. It is a MAO inhibitor, antagonizes the response to tyramine and blocks neuronal uptake of noradrenaline.
Cas No.:30578-37-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Amezinium is a sympathomimetic used for its vasopressor effects in the treatment of hypotensive states. It is a MAO inhibitor, antagonizes the response to tyramine and blocks neuronal uptake of noradrenaline.
| Cas No. | 30578-37-1 | SDF | |
| 别名 | 甲磺美嗪,Amezinium metilsulfate; Lu-1631 | ||
| Canonical SMILES | COC1=CC(N)=CN=[N+]1C2=CC=CC=C2.O=S(OC)([O-])=O | ||
| 分子式 | C12H15N3O5S | 分子量 | 313.33 |
| 溶解度 | DMSO : ≥ 34 mg/mL (108.51 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 | 3.1915 mL | 15.9576 mL | 31.9152 mL |
| 5 mM | 0.6383 mL | 3.1915 mL | 6.383 mL |
| 10 mM | 0.3192 mL | 1.5958 mL | 3.1915 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。
Amezinium metilsulfate, a sympathomimetic agent, may increase the risk of urinary retention in multiple system atrophy
Clin Auton Res 2003 Feb;13(1):51-3.PMID:12664248DOI:10.1007/s10286-003-0034-5.
In 5 patients with multiple system atrophy, administration of 15 mg/day of Amezinium metilsulfate, an adrenergic agent, during 6 months for the treatment of postural hypotension exacerbated post-micturition residuals as compared to that before treatment (178 ml versus 113 ml for a change of 37 %, p < 0.05). Amezinium metilsulfate most probably stimulates both alpha1B-receptors in the vascular wall and alpha1A/D-receptors in the proximal urethra.
Treatment of neurogenic orthostatic hypotension with Amezinium metilsulfate, a new indirect sympathomimetic drug
Neurology 1988 Jul;38(7):1095-9.PMID:3386828DOI:10.1212/wnl.38.7.1095.
Amezinium metilsulfate is a new, indirectly acting sympathomimetic drug which exclusively affects postganglionic sympathetic neurons and inhibits both intraneuronal monoamine oxidase and norepinephrine reuptake. We examined the short-term effects of amezinium in five patients with severe neurogenic orthostatic hypotension. Single-dose administration of amezinium (10 mg) raised both the supine and sitting mean blood pressures by 15 to 45 mm Hg for 8 hours, with a slight increase in the plasma norepinephrine level. Repeated administration of amezinium (10 to 40 mg/d) produced an increase in sitting blood pressure in three patients and improvement of the orthostatic symptoms in all patients without remarkable recumbent hypertension. The heart rate was increased in two patients. The results indicate that amezinium is of therapeutic value for the treatment of neurogenic orthostatic hypotension. The adrenergic effect of amezinium on the blood pressure and heart rate apparently was related to a slight increase in endogenous norepinephrine in the presence of alpha- and beta-adrenoreceptor supersensitivity.
Effect of Amezinium metilsulfate on the finger skin vasoconstrictor response to cold stimulation and venoconstrictor response to noradrenaline
Jpn Circ J 1998 Nov;62(11):824-8.PMID:9856598DOI:10.1253/jcj.62.824.
Orthostatic hypotension can be caused by an inadequate vasoconstrictor response. The effects of amezinium on vasoconstrictor response to sympathetic stimulation and to exogenous noradrenaline were investigated and compared with those of midodrine. In 8 healthy men, the following experiments were performed after a single oral dose of 10mg of amezinium, 2mg of midodrine or a placebo. First, finger-tip blood flow (FTBF) was recorded using a laser Doppler flowmeter before and during the contralateral hand cooling and a reduction ratio of FTBF was calculated as an index of the vasoconstrictor response. Second, dose-response curves to increasing doses (1-512ng/min) of noradrenaline infused locally to the dorsal hand vein were determined using a linear variable differential transformer. The reduction ratio of FTBF was significantly increased (p<0.05) by amezimium [placebo, 75.9 +/- 9.8(mean +/- SD)%; amezinium, 85.1 +/- 7.9%; midodrine, 78.1 +/- 9.3%]. The infusion rate of noradrenaline producing a half-maximum venoconstriction was significantly decreased (p<0.05) by amezinium (placebo, 40.6 +/- 33.9 ng/min; amezinium, 21.0 +/- 21.3 ng/min; midodrine, 33.2 +/- 31.5 ng/min). These findings indicate that amezinium increases the vasoconstrictor response to sympathetic stimulation and to noradrenaline in normal subjects, and this mechanism might contribute to the improvement by amezinium of the symptoms of orthostatic hypotension.
Diffuse cerebrovascular dilation: Case report of amezinium metilsulfate-induced reversible cerebral vasoconstriction syndrome
Cephalalgia 2016 Mar;36(3):289-93.PMID:26016487DOI:10.1177/0333102415588326.
Background: Reversible cerebral vasoconstriction syndrome (RCVS) is characterized by recurrent thunderclap headaches with reversible cerebral vasoconstriction, and often precipitated by the postpartum state and vasoactive medications. We describe a case of a patient with RCVS induced by Amezinium metilsulfate, a sympathomimetic drug, in whom magnetic resonance angiography (MRA) initially revealed diffusely dilated cerebral arteries. Case description: A 34-year-old woman was prescribed Amezinium metilsulfate for hypotension. Twelve days later, she suffered from abrupt severe headaches and was referred to our department. She had no neurological deficits; however, MRA revealed diffusely dilated anterior, middle, and posterior cerebral arteries with vasoconstriction. She was tentatively diagnosed with RCVS and successfully treated with verapamil for headache. Nevertheless, follow-up MRAs disclosed widespread segmental vasoconstriction that resolved in two months. Discussion: Diffuse cerebrovascular dilation has not been addressed but may be associated with RCVS pathophysiology. In addition, physicians should bear in mind that Amezinium metilsulfate can potentially induce RCVS.
[Effects of oral Amezinium metilsulfate in patients with sick sinus syndrome]
J Cardiol 1997 Jul;30(1):29-35.PMID:9253693doi
The effects of Amezinium metilsulfate (Risumic) were studied in patients with sick sinus syndrome. Four males and 11 females with clinical symptoms were treated with 0.5 mg/kg for 1 to 40 weeks. In all patients, the length of sinus pause observed during 24-hour Holter monitoring was longer than 2.0 sec, and/or the sinus node recovery time in the electrophysiologic study was longer than 2.0 sec. The effects were evaluated by Holter monitoring and standard electrocardiography. The total number of heart beats every 24 hours by Holter monitoring were significantly increased from 78,917 +/- 15,983 (mean +/- SD) to 85,753 +/- 17,849 beats after the treatment. The length of the sinus pause was significantly decreased from 3.89 +/- 1.24 to 2.36 +/- 1.45 sec. Patients with sinus node recovery time of less than 5.0 sec showed the effects especially clearly. The total number of premature ventricular contractions was decreased from 530 +/- 767 to 123 +/- 182 beats. The PQ, QRS and QTc intervals did not change. Only diastolic pressure was slightly increased. Clinical symptoms disappeared in almost all patients and the clinical courses were favorable. Amezinium metilsulfate, which stimulates the intrinsic sympathetic nervous system, increased total heart beat and shortened sinus pause in patients with sick sinus syndrome. Few side effects, such as arrhythmogenecity or increase of blood pressure were observed. These results show that Amezinium metilsulfate is useful in the treatment of patients with sick sinus syndrome, if the disease is not so severe as to require implantation of a cardiac pacemaker.