Metyrosine
(Synonyms: 甲酪氨酸) 目录号 : GC41634
An inhibitor of tyrosine hydroxylase
Cas No.:672-87-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Metyrosine is an inhibitor of tyrosine hydroxylase. In vivo, metyrosine (200 mg/kg) reduces norepinephrine and dopamine levels in rat brain and disrupts conditioned avoidance behavior in a dose-dependent manner. Metyrosine reduces dopamine transporter knockdown-induced hyperactivity and rearing behavior and increases exploratory behavior in a hole board assay in a mouse model of bipolar disorder mania. It reduces hypertension induced by dexamethasone and cyclosporin in rats. Metyrosine also inhibits norepinephrine production and increases plasma levels of leptin in fasted and fed mice.
| Cas No. | 672-87-7 | SDF | |
| 别名 | 甲酪氨酸 | ||
| Canonical SMILES | OC1=CC=C(C[C@](N)(C)C(O)=O)C=C1 | ||
| 分子式 | C10H13NO3 | 分子量 | 195.2 |
| 溶解度 | DMF: <50 µ g/ml,DMSO: <50 µ g/ml,Ethanol: <50 µ g/ml,PBS (pH 7.2): >2 mg/ml | 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 | 5.123 mL | 25.6148 mL | 51.2295 mL |
| 5 mM | 1.0246 mL | 5.123 mL | 10.2459 mL |
| 10 mM | 0.5123 mL | 2.5615 mL | 5.123 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。
The Role for Metyrosine in the Treatment of Patients With Pheochromocytoma and Paraganglioma
J Clin Endocrinol Metab 2021 May 13;106(6):e2393-e2401.PMID:33693908DOI:10.1210/clinem/dgab130.
Context: Treatment of pheochromocytoma and paraganglioma (PPGL) requires preintervention titration of alpha- and beta-adrenergic blockade, but patients may still be at risk for complications from catecholamine excess. Metyrosine decreases catecholamine production, making it an attractive therapeutic adjunct for select patients. Evidence acquisition: A systematic literature review was performed (Ovid Medline and Scopus databases) on December 17, 2019, including studies with humans and original data. Studies with 10 or more patients on Metyrosine for PPGL were included. Studies were screened for overlapping populations, and the most comprehensive study was included. The references of included studies were reviewed for additional data. Patient data from our institution between 2000 and 2015 were also reviewed. Evidence synthesis: Metyrosine is well tolerated when used for a short course and can improve intraoperative outcomes in PPGL. Metyrosine should be considered when a difficult PPGL resection is expected (eg, pericardiac paraganglioma, abdominal paraganglioma with great vessel involvement), a large release of catecholamines is anticipated (eg, ablative therapy, chemotherapy), or when standard alpha- and beta-adrenergic blockade are not tolerated or cannot adequately control hypertension. Side effects are generally mild and self-limited, with sedation in a majority of patients. Extrapyramidal side effects are rare but can limit use of Metyrosine. Because of its expense and limited availability, Metyrosine use should be carefully planned and timed in relation to surgery. Conclusions: Metyrosine is a safe addition to traditional alpha- and beta-adrenergic blockade and should be considered in those patients with PPGL at high risk for acute release of catecholamines.
Metyrosine and pheochromocytoma
Arch Intern Med 1997 Apr 28;157(8):901-6.PMID:9129550doi
Background: Severe hemodynamic instability may occur during surgery for removal of pheochromocytoma, unless there is preoperative pharmacological treatment. Objective: To evaluate the effects of Metyrosine (alpha-methyl-p-tyrosine), a catecholamine synthesis inhibitor, and alpha-blockade with prazosin or phenoxybenzamine on cardiovascular morbidity during surgery for pheochromocytoma. Methods: A retrospective analysis was made of patients followed up at the Medical College of Georgia, Augusta, during 28 years who received Metyrosine and prazosin (n = 6), Metyrosine and phenoxybenzamine alone (n = 14), phenoxybenzamine alone (n = 6), or no medication (n = 7) during 3 weeks before tumor removal. The percentage of patients not requiring pressors or phentolamine during the intraoperative period as well as the perioperative peak systolic pressures and peak heart rates were estimated in each group. Results: There was a significant (P < .05) increase in intraoperative peak systolic pressures without preoperative treatment (mean +/- SD, 243 +/- 40 mm Hg) vs Metyrosine (mean +/- SD, 168 +/- 27 mm Hg). Ninety-five percent of patients who received Metyrosine did not require pressors intraoperatively vs 50% with phenoxybenzamine alone. Eighty-one percent of patients pretreated with Metyrosine did not require intraoperative phentolamine vs 33% with phenoxybenzamine alone and 29% without medications. Two patients in the no medication group died as a results of hypertensive crisis. Conclusions: The combination of alpha-metyrosine and alpha-blockade results in better blood pressure control and less need for use of antihypertensive medication or pressors during surgery, compared with the classical method of single-agent adrenergic blockade. Preoperative treatment with Metyrosine along with an alpha-blocker is a useful strategy for decreasing the surgical morbidity in patients with pheochromocytoma and assumes greater importance as long as the availability of phentolamine for intraoperative use is a problem.
Efficacy and safety of Metyrosine in pheochromocytoma/paraganglioma: a multi-center trial in Japan
Endocr J 2018 Mar 28;65(3):359-371.PMID:29353821DOI:10.1507/endocrj.EJ17-0276.
To assess the efficacy, safety, and pharmacokinetics of Metyrosine (an inhibitor of catecholamine synthesis) in patients with pheochromocytoma/paraganglioma (PPGL), we conducted a prospective, multi-center, open-label study at 11 sites in Japan. We recruited PPGL patients aged ≥12 years requiring preoperative or chronic treatment, receiving α-blocker treatment, having baseline urinary metanephrine (uMN) or normetanephrine (uNMN) levels ≥3 times the upper limit of normal values, and having symptoms associated with excess catecholamine. Metyrosine treatment was started at 500 mg/day and modified according to dose-adjustment criteria up to 4,000 mg/day. The main outcome measure was the proportion of patients who achieved at least 50% reduction in uMN or uNMN levels from baseline. Sixteen patients (11 males/5 females) aged 12-86 years participated. After 12 weeks of treatment and at the last evaluation of efficacy, the primary endpoint was achieved in 31.3% of all patients, including 66.7% of those under preoperative treatment and 23.1% of those under chronic treatment. Sedation, anemia, and death were reported in 1 patient each as serious adverse drug reactions during the 24-week treatment. Metyrosine was shown to be tolerated and to relieve symptoms by reducing excess catecholamine in PPGL patients under both preoperative and chronic treatment.
Preoperative Metyrosine Improves Cardiovascular Outcomes for Patients Undergoing Surgery for Pheochromocytoma and Paraganglioma
Ann Surg Oncol 2015 Dec;22 Suppl 3:S646-54.PMID:26374407DOI:10.1245/s10434-015-4862-z.
Background: The goal of preoperative pharmacotherapy for pheochromocytoma (PCC) and paraganglioma (PGL) resection is to minimize intraoperative hemodynamic instability and perioperative cardiovascular complications, but no standard preoperative regimen exists. Historically, treatment used Metyrosine and phenoxybenzamine (MP). The recent Metyrosine shortage required that phenoxybenzamine alone (PA) be used for treatment. The authors examined their experience to determine the impact of preoperative Metyrosine treatment on patient outcomes. Methods: A retrospective cohort study investigated patients who underwent initial PCC/PGL resection (2000-2014). The primary outcome was intraoperative hemodynamics, measured by heart rate (HR) and systolic blood pressure (SBP). The secondary outcomes included perioperative complications and cardiovascular-specific complications (CVC). Univariate analysis was performed, and adjusted risk differences were estimated after confounding was taken into account. Results: Of 174 patients, 142 (81.6 %) were in the MP group. The MP and PA patients had comparable intraoperative use of antihypertensives (83.9 vs 78.1 %; p = 0.443), vasopressors (74.6 vs 87.5 %; p = 0.120), and fluid resuscitation (mean, 24.4 vs 24.8 ml/min; p = 0.761). Although the perioperative complication rate did not differ significantly between the MP and PA groups (respectively 23.4 vs 34.4 %; p = 0.198), the PA patients had a 15.8 % higher rate of CVC even after controlling for confounders (p = 0.034). Compared with the MP patients, the PA patients had significantly more hemodynamic instability intraoperatively, with a greater range in HR (7.4 bpm; p = 0.034) and SBP (14.8 mmHg; p = 0.020). Conclusions: In this study, preoperative Metyrosine improved intraoperative hemodynamic stability and decreased CVC rates in patients undergoing PCC/PGLresection. These data suggest that the addition of preoperative Metyrosine may improve operative outcomes.
The effects of Metyrosine on ischemia-reperfusion-induced oxidative ovarian injury in rats: Biochemical and histopathological assessment
An Acad Bras Cienc 2023 Apr 3;95(2):e20201586.PMID:37018835DOI:10.1590/0001-3765202320201586.
The aim of this study is to investigate the effect of Metyrosine on ischemia-reperfusion (I/R) induced ovarian injury in rats in terms of biochemistry and histopathology. Rats were divided into: ovarian I/R (OIR), ovarian I/R+50 mg/kg Metyrosine (OIRM) and sham (SG) operations. OIRM group received 50 mg/kg Metyrosine one hour before the application of the anesthetic agent, OIR and SG group rats received equal amount of distilled water to be used as a solvent orally through cannula. Following the application of the anesthetic agent, ovaries of OIRM and OIR group rats were subjected to ischemia and reperfusion, each of which took two hours. This biochemical experiment findings revealed high levels of malondialdehyde (MDA) and cyclo-oxygenase-2 (COX-2) and low levels of total glutathione (tGSH), superoxide dismutase (SOD) and cyclo-oxygenase-1 (COX-1) in the ovarian tissue of OIR group, with significant histopathological injury. In Metyrosine group, MDA and COX-2 levels were lower than the OIR group whereas tGSH, SOD and COX-1 levels were higher, with slighter histopathological injury. Our experimental findings indicate that Metyrosine inhibits oxidative and pro-inflammatory damage associated with ovarian I/R in rats. These findings suggest that Metyrosine could be useful in the treatment of ovarian injury associated with I/R.