Toloxatone
(Synonyms: 托洛沙酮; MD 69276) 目录号 : GC34842
An inhibitor of MAO-A
Cas No.:29218-27-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Toloxatone is an inhibitor of monoamine oxidase A (MAO-A; Ki = 1.8 ?M).1 It is selective for MAO-A over MAO-B (Ki = 44 ?M). Toloxatone (100 mg/kg) inhibits deamination of serotonin (5-HT) and norepinephrine in rat brain.2 It also decreases immobility time in the forced swim test in mice when administered at a dose of 256 mg/kg.3
1.Cesura, A.M., and Pletscher, A.The new generation of monoamine oxidase inhibitorsProg. Drug Res.38171-297(1992) 2.Keane, P.E., Kan, J.P., Sontag, N., et al.Monoamine oxidase inhibition and brain amine metabolism after oral treatment with toloxatone in the ratJ. Pharm. Pharmacol.31(11)752-754(1979) 3.Van der Meersch-Mougeot, V., da Rocha, M., Jr., Monier, C., et al.Benzodiazepines reverse the anti-immobility effect of antidepressants in the forced swimming test in miceNeuropharmacology32(5)439-446(1993)
| Cas No. | 29218-27-7 | SDF | |
| 别名 | 托洛沙酮; MD 69276 | ||
| Canonical SMILES | CC1=CC(N2C(OC(CO)C2)=O)=CC=C1 | ||
| 分子式 | C11H13NO3 | 分子量 | 207.23 |
| 溶解度 | DMSO : 125 mg/mL (603.19 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 | 4.8256 mL | 24.1278 mL | 48.2556 mL |
| 5 mM | 0.9651 mL | 4.8256 mL | 9.6511 mL |
| 10 mM | 0.4826 mL | 2.4128 mL | 4.8256 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 | ||||||||||
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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。
Toloxatone pharmacokinetics in the plasma and cerebrospinal fluid of the rabbit
J Pharm Pharmacol 1992 Feb;44(2):124-6.PMID:1352813DOI:10.1111/j.2042-7158.1992.tb03576.x.
The pharmacokinetics of Toloxatone (5 and 10 mg kg-1, i.v.) was studied in anaesthetized rabbits. There was a biexponential decline in plasma concentration with time. No differences were observed in the pharmacokinetic parameters with the increase of the dose. The terminal half-life was short (47.4 +/- 2.8 and 41.5 +/- 4.2 min for 5 and 10 mg kg-1, respectively). The total clearance was 79 +/- 18 mL min-1 after a dose of 5 mg kg-1 and 106 +/- 40 mL min-1 after a dose of 10 mg kg-1. The volume of distribution was 5.8 +/- 2.8 (5 mg kg-1) and 5.4 +/- 1.8 L (10 mg kg-1). The average percentage of Toloxatone bound to plasma protein was 30% and was not affected by concentrations within the investigated range. In cerebrospinal fluid (CSF), the highest concentrations of Toloxatone were obtained within 15 min after the end of the injection. The CSF level of Toloxatone was equal to that of plasma unbound Toloxatone and declined at a rate similar to Toloxatone in plasma. These results suggest that the Toloxatone passage through the blood-brain barrier may be completed by passive diffusion. In addition, the unbound plasma concentration would accurately reflect the Toloxatone concentration in CSF and could be a useful tool for drug monitoring.
[Toloxatone and depression]
Acta Psiquiatr Psicol Am Lat 1991 Dec;37(4):291-8.PMID:1843597doi
One hundred and one depressed inpatients were treated by the authors with a second-generation antidepressive original molecule: Toloxatone, a specific and reversible MAO A inhibitor. Upon admission, all 101 patients with depressive illness did not score higher than 20 on Hamilton's Scale, and did not score lower than 4 on Fischer, Fernández Labriola and Rodríguez Casanova's Endogeneity Test. Biological profiles (Phenyl-ethylamine, NA, and MHPG) were available on 57 subjects. At the beginning of the experiment: (a) No subject was taking antidepressives, (b) Patients' age averaged 46; (c) The 6-week experiment was a double-blind vs. placebo type. Daily Toloxatone dose was standardized in a 400 mg intake. Significant modifications were detected in 51 subjects. Among the 59 subjects that were administered active substance, 37 achieved either "excellent" or "good" outcomes. Biological markers pointed out a profile of patients with a better response to Toloxatone: Namely, patients with a lower noradrenergic activity. Anxiety-free depression as well as inhibited depressions are a psychiatrist's choice for administering Toloxatone.
Pharmacokinetic and pharmacodynamic interaction between Toloxatone, a new reversible monoamine oxidase-A inhibitor, and oral tyramine in healthy subjects
Clin Pharmacol Ther 1992 Oct;52(4):384-93.PMID:1424410DOI:10.1038/clpt.1992.159.
We examined the influence of Toloxatone, a new reversible monoamine oxidase-A inhibitor used in the treatment of depression, on tyramine-induced pressor effect in healthy volunteers. The maximum increase in systolic blood pressure produced by four single oral doses of tyramine administered during a meal and ranging from 100 mg to 800 mg was compared during repeated (3 to 5 days) administration of placebo, 200 mg Toloxatone three times a day and 400 mg Toloxatone three times a day in a single-blind, three-period crossover study. Toloxatone by itself had no significant influence on blood pressure. During administration of Toloxatone, no significant increase in tyramine-induced increase in systolic blood pressure was observed for tyramine doses of 200 mg or less that are consistently higher than those associated with normal food intake. However, Toloxatone increased the tyramine-induced increase in blood pressure after 400 mg tyramine (400 mg Toloxatone three times a day) and 800 mg tyramine (200 mg Toloxatone three times a day and 400 mg Toloxatone three times a day). This pharmacodynamic interaction could be explained by an increase in tyramine systemic bioavailability in the presence of Toloxatone. It is concluded that interaction between tyramine in meals and Toloxatone is unlikely to occur in patients after long-term administration of the drug at therapeutic dosages.
Characterization of forced degradation products of Toloxatone by LC-ESI-MS/MS
Saudi Pharm J 2018 May;26(4):467-480.PMID:29844717DOI:10.1016/j.jsps.2018.02.012.
Forced degradation of Toloxatone in solutions under basic, acidic, neutral, photo UV-VIS, photo UVC and oxidative stress conditions was investigated and structural elucidation of its degradation products was performed with the use of UHPLC system coupled ESI-Q-TOF mass spectrometer. Eight degradation products were found and their masses and formulas were obtained with high accuracy (0.09-3.79 ppm). The structure of unknown degradation products were elucidated from MS/MS fragmentation spectra of all analyzed compounds. Additionally, whole signals of decomposed substances were compared chemometrically. It was found that Toloxatone is fragile towards basic hydrolysis, oxidative conditions and UVC irradiation. Finally, the toxicity of transformation products was computationally evaluated and compared in multivariate manner.
A double-blind comparison of moclobemide and Toloxatone in out-patients presenting a major depressive disorder
Psychopharmacology (Berl) 1992;106 Suppl:S118-9.PMID:1546124DOI:10.1007/BF02246253.
A double-blind comparison of moclobemide and Toloxatone was performed in adult out-patients diagnosed as suffering from a major depressive disorder. Parallel groups of patients received moclobemide, 450 mg/day (n = 135) or Toloxatone, 1000 mg/day (n = 133) for 28 days. Both groups showed a significant clinical improvement while on therapy; the response was most marked and rapid in those receiving moclobemide treatment. Improvement was greatest in those patients with the most severe depression at the time of trial onset. A significantly higher number of patients returned to normal sleep patterns following moclobemide treatment than following Toloxatone. Overall, tolerance was rated as good or very good in more than 80% of patients. The most frequent complaints in the moclobemide-treated group were hot flushes, dry mouth, constipation and headache, while an increase in anxiety was associated with Toloxatone usage. Moclobemide was found to be as effective as Toloxatone in the treatment of major depressive episodes, but with the advantages of improved sleep patterns and reduced anxiety.