Nomifensine maleate
(Synonyms: 诺米芬新马来酸盐; (±)-Nomifensine maleat) 目录号 : GC64381
An inhibitor of norepinephrine and dopamine reuptake
Cas No.:32795-47-4
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
Nomifensine is an inhibitor of norepinephrine (NE) and dopamine (DA) reuptake.1 It inhibits uptake of NE, DA, and serotonin (5-HT) in rat brain synaptosomes with IC50 values of 6.6, 48, and 830 nM, respectively. It is selective for DA, NE, and 5-HT uptake inhibition over binding to dopamine D2, α1- adrenergic-, 5-HT2, and muscarinic receptors (IC50s = 43,000, 1,200, 3,800, and >13,000 nM, respectively, in rat brain membranes). Nomifensine is selective for inhibition of NE over DA uptake in vivo with minimal inhibitory doses of 28 and less than 57 ?mol/kg, respectively. It decreases the time Wistar Kyoto, but not Sprague-Dawley, rats spend immobile in the forced swim test but also increases locomotor activity in the open field test in Wistar Kyoto and Sprague-Dawley rats when administered at a chronic dose of 10 mg/kg.2
1.Hyttel, J., and Larsen, J.J.Neurochemical profile of Lu 19-005, a potent inhibitor of uptake of dopamine, noradrenaline, and serotoninJ. Neurochem.44(5)1615-1622(1985) 2.Tejani-Butt, S., Kluczynski, J., and Paré, W.P.Strain-dependent modification of behavior following antidepressant treatmentProg. Neuropsychopharmacol. Biol. Psychiatry27(1)7-14(2003)
| Cas No. | 32795-47-4 | SDF | Download SDF |
| 别名 | 诺米芬新马来酸盐; (±)-Nomifensine maleat | ||
| 分子式 | C20H22N2O4 | 分子量 | 354.4 |
| 溶解度 | DMSO : ≥ 80 mg/mL (225.73 mM)|Water : 2.2 mg/mL (6.21 mM; Need ultrasonic) | 储存条件 | 4°C, away from moisture |
| 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 | 2.8217 mL | 14.1084 mL | 28.2167 mL |
| 5 mM | 0.5643 mL | 2.8217 mL | 5.6433 mL |
| 10 mM | 0.2822 mL | 1.4108 mL | 2.8217 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 | ||||||||||
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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。
Nomifensine maleate (Merital, Hoechst-Roussel)
Drug Intell Clin Pharm 1982 Jul-Aug;16(7-8):547-52.PMID:7049645DOI:10.1177/106002808201600703.
Nomifensine is an isoquinoline antidepressant that inhibits the reuptake of dopamine at central synapses. It also inhibits norepinephrine reuptake but is only a weak inhibitor of 5-hydroxytryptamine. Open and controlled trials comparing nomifensine with placebo and other standard antidepressants have shown it to be an effective antidepressant in divided doses up to 200 mg/d. The full dosage range of 50-200 mg/d is well tolerated, and doses can be selected to suit patient disease, age, and therapeutic response. Minimal anticholinergic and sedative side effects and no impairment of psychomotor performance make nomifensine a suitable drug for use in a wide variety of ambulatory outpatients, including the elderly. A relative lack of cardiotoxicity and epileptogenic activity add to this profile; the safety of the drug, when taken in overdose, has been documented. However, the place of nomifensine in the treatment of depression, relative to other antidepressants, is still unclear.
Nomifensine maleate: a new second-generation antidepressant
Clin Pharm 1985 Nov-Dec;4(6):625-36.PMID:3907935doi
The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, dosage, and formulary recommendations for Nomifensine maleate are reviewed. Nomifensine is a potent inhibitor of norepinephrine but has little effect on serotonin. It is unique in that it is a potent reuptake inhibitor of dopamine. Nomifensine is rapidly and completely absorbed and is widely distributed throughout the body. The major route of elimination is through the kidneys. Because of its short half-life and resultant lack of accumulation, nomifensine is usually given in divided doses. Nomifensine is approved for the treatment of depression. In clinical trials with imipramine, amitriptyline, nortriptyline, maprotiline, and various investigational antidepressant drugs, it has been found to be as effective as the standard antidepressant agents. In general, nomifensine has been well tolerated by patients and has caused few side effects. It also has not been associated with serious toxic effects in overdose situations. The usual effective dose of Nomifensine maleate is 100-200 mg daily given in divided doses. It appears to be a good choice for patients with profoundly retarded depression and for those who cannot tolerate the side effects of traditional antidepressant drugs. Nomifensine should not be used alone in patients with schizoaffective disorders or in patients with agitated depression. Nomifensine is a safe and effective antidepressant with a fairly unique pharmacological profile. Because the drug is relatively safe and causes little sedation, it may offer substantial advantages over the more traditional antidepressants and should be considered for formulary addition.
Nomifensine maleate in adult attention deficit disorder
J Nerv Ment Dis 1989 May;177(5):296-9.PMID:2651559DOI:10.1097/00005053-198905000-00008.
The authors studied 18 adults (8 men and 10 women) in an open trial of Nomifensine maleate for the treatment of attention deficit disorder (ADD). All patients met DSM-III criteria and the Utah criteria for ADD, residual type (RT). Medication effect was measured at week 1 and week 4 of treatment using the Structured Interview for ADD-H Symptoms. Data from week 4 showed that all eight men and seven of the women responded well to nomifensine, showing a significant decrease in ADD with hyperactivity symptoms. Side effects were minimal, consisting of drowsiness, dry mouth, headache, and nausea. One responder (5%) was taken off the medicine after developing an allergic reaction. Results showed that short-term use of nomifensine was relatively free from side effects and was remarkably effective in the treatment of ADD-RT. The authors discussed the implications of the use of nomifensine and related drugs in the treatment of ADD-RT.
Kinetics and metabolism of nomifensine
J Clin Psychiatry 1984 Apr;45(4 Pt 2):21-5.PMID:6370971doi
Metabolic and pharmacokinetic studies of Nomifensine maleate, a tetrahydroisoquinoline derivative with antidepressant properties, are reviewed. Results of pharmacokinetic studies indicate that nomifensine has a short distribution phase and a large volume of distribution. It is rapidly metabolized to its N-glucuronide. Plasma levels of nomifensine-N-glucuronide are up to 100-fold higher than those of nomifensine, obviously because of a smaller volume of distribution. As nomifensine-N-glucuronide is extremely unstable and cleaved to nomifensine, determinations of nomifensine are easily falsified. It is therefore recommended only to determine the sum of nomifensine and its N-glucuronide (total nomifensine) in clinical trials. Kinetics of total nomifensine can best be described by the open two-compartment model: Maximum plasma levels are obtained 1-2 hours postadministration; mean elimination half-life is 2 hours. Excretion is almost entirely by the kidneys, with approximately 88% of an oral dose excreted within 24 hours.
The pharmacokinetics and bioavailability of Nomifensine maleate in healthy men
J Clin Psychiatry 1984 Apr;45(4 Pt 2):26-32.PMID:6715299doi
Two studies were conducted in normal male volunteers to establish the pharmacokinetic parameters for Nomifensine maleate and to determine the bioavailability of the drug from the Merital capsule intended for U.S. marketing. Single oral doses of 25, 100, and 200 mg of Nomifensine maleate as aqueous solutions were administered to 24 men in the open-label Latin-square design pharmacokinetic study. In the bioavailability study, 24 men received single oral 50 mg doses of Nomifensine maleate in a capsule or as an aqueous solution. Plasma levels of nomifensine were determined by radioimmunoassay and urinary levels of total nomifensine and its metabolites were assayed by thin-layer chromatography. There was a proportional increase in the area under the curve (AUC) with increasing dose, while peak plasma levels and amounts of total nomifensine and its metabolites excreted in the urine rose as dose increased. The pharmacokinetics of nomifensine are considered linear over the dose range tested. Nomifensine maleate was equally bioavailable from the 50 mg aqueous solution and the Merital capsule formulation.