Isocarboxazid
(Synonyms: 异卡波肼) 目录号 : GC31104
An inhibitor of MAO
Cas No.:59-63-2
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
Isocarboxazid is an inhibitor of monoamine oxidase (MAO; IC50 = 4.8 μM for rat brain MAO).1 It induces a 4-fold increase in tryptamine action in isolated rat fundal strips at a concentration of 50 nM. In vivo, isocarboxazid potentiates tryptamine toxicity (LD50 = 8 mg/kg following subcutaneous administration of 250 mg/kg tryptamine). It inhibits 90% of MAO activity in isolated rat hearts and reduces cardiomegaly induced by isoproterenol in rats at a dose of 20 mg/kg.2 Oral administration of isocarboxazid (10 mg/kg) increases levels of dopamine and norepinephrine and reduces levels of the monoamine metabolites DOPAC, homovanillic acid , and 5-hydroxy indole-3-acetic acid by 43, 32, and 28%, respectively, in mouse brain.3 Formulations containing isocarboxazid have been used for the treatment of minor depression.4
1.Maxwell, D.R., Gray, W.R., and Taylor, E.M.Relative activity of some inhibitors of mono-amine oxidase in potentiating the action of tryptamine in vitro and in vivoBr. J. Pharmacol. Chemother.17(3)310-320(1961) 2.Stanton, H.C., Bowman, Z., and Cooper, C.M.Effects of monoamine oxidase inhibitors on isoproterenol-induced cardiomegaly in ratsToxicol. Appl. Pharmacol.16(1)256-263(1970) 3.Yokoyama, T., Kamioka, T., Iwata, N., et al.Effects of RS-2232, a potential antidepressant, on the levels of monoamines, precursor amino acids and their related metabolites in mouse brainJpn. J. Pharmacol.44(4)413-420(1987) 4.Barbui, C., Cipriani, A., Patel, V., et al.Efficacy of antidepressants and benzodiazepines in minor depression: Systematic review and meta-analysisBr. J. Psychiatry198(1)11-16(2011)
| Cas No. | 59-63-2 | SDF | |
| 别名 | 异卡波肼 | ||
| Canonical SMILES | O=C(C1=NOC(C)=C1)NNCC2=CC=CC=C2 | ||
| 分子式 | C12H13N3O2 | 分子量 | 231.25 |
| 溶解度 | Acetonitrile: Slightly Soluble,Chloroform: Slightly Soluble | 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 | 4.3243 mL | 21.6216 mL | 43.2432 mL |
| 5 mM | 0.8649 mL | 4.3243 mL | 8.6486 mL |
| 10 mM | 0.4324 mL | 2.1622 mL | 4.3243 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。
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Isocarboxazid
Isocarboxazid is a monoamine oxidase inhibitor (MAO inhibitor) used in therapy of severe depression. Isocarboxazid therapy is associated with rare instances of clinically apparent acute liver injury.
Isocarboxazid
Because of the lack of data on use during breastfeeding, other antidepressants are preferred during breastfeeding.
The prescriber's guide to classic MAO inhibitors (phenelzine, tranylcypromine, isocarboxazid) for treatment-resistant depression
This article is a clinical guide which discusses the "state-of-the-art" usage of the classic monoamine oxidase inhibitor (MAOI) antidepressants (phenelzine, tranylcypromine, and isocarboxazid) in modern psychiatric practice. The guide is for all clinicians, including those who may not be experienced MAOI prescribers. It discusses indications, drug-drug interactions, side-effect management, and the safety of various augmentation strategies. There is a clear and broad consensus (more than 70 international expert endorsers), based on 6 decades of experience, for the recommendations herein exposited. They are based on empirical evidence and expert opinion-this guide is presented as a new specialist-consensus standard. The guide provides practical clinical advice, and is the basis for the rational use of these drugs, particularly because it improves and updates knowledge, and corrects the various misconceptions that have hitherto been prominent in the literature, partly due to insufficient knowledge of pharmacology. The guide suggests that MAOIs should always be considered in cases of treatment-resistant depression (including those melancholic in nature), and prior to electroconvulsive therapy-while taking into account of patient preference. In selected cases, they may be considered earlier in the treatment algorithm than has previously been customary, and should not be regarded as drugs of last resort; they may prove decisively effective when many other treatments have failed. The guide clarifies key points on the concomitant use of incorrectly proscribed drugs such as methylphenidate and some tricyclic antidepressants. It also illustrates the straightforward "bridging" methods that may be used to transition simply and safely from other antidepressants to MAOIs.
Isocarboxazid--Marplan
Treatment History Characteristics Associated With Use of Isocarboxazid: A Nationwide Register-Based Study
Purpose/background: The monoamine oxidase inhibitor isocarboxazid (Marplan) is occasionally used in the treatment of depression, but there is only little knowledge on the nature of the use of isocarboxazid in clinical practice. We aimed to identify treatment history characteristics associated with this use.
Methods/procedures: Via the nationwide Danish registers, we identified all adult incident users of isocarboxazid in the period from 2001 to 2018, as well as up to 5 matched controls using another antidepressant (matched on date of redeemed prescription, age, sex, and region of residence). The 5-year treatment history of the isocarboxazid users and the controls was assessed via the Danish registers. The association between treatment history characteristics and isocarboxazid use was examined by multivariate conditional logistic regression.
Findings/results: We identified 1455 isocarboxazid users and 7045 controls using another antidepressant. The following characteristics were associated with statistically significant increased likelihood of receiving isocarboxazid treatment: Prior treatment with a selective serotonin reuptake inhibitor (odds ratio [OR], 1.80 with 95% confidence interval [CI], 1.46-2.23), a serotonin-norepinephrine reuptake inhibitor (OR, 4.90; 95% CI, 4.08-5.89), a noradrenergic and specific serotonergic antidepressant (OR, 1.56; 95% CI, 1.30-1.88), a tricyclic antidepressant (OR, 5.05; 95% CI, 4.19-6.08), other antidepressants (OR, 4.74; 95% CI, 3.74-6.01), lithium (OR, 6.70; 95% CI, 5.08-8.83), an antipsychotic (OR, 1.43; 95% CI, 1.19-1.73), and each diagnosis of depression received in relation to psychiatric hospital treatment (OR, 1.31; 95% CI, 1.23-1.39). Forty percent of those initiating isocarboxazid had received treatment with drugs from 5 or more different psychopharmacological classes in the 5 preceding years.
Implications/conclusions: These findings suggest that isocarboxazid is typically used for treatment-resistant depression, consistent with guideline recommendations.