| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
/Other Toxicity Information/ In two independent trials, a healthy male volunteer was orally (PO) administered the monoamine oxidase inhibitor nialamide (total intake of 300 mg and 1000 mg, respectively), and urinary bufotenine excretion was monitored via continuous urine sampling. In both trials, nialamide excretion was significantly higher than that in the same subject without nialamide (median 0.089 nmol/mmol creatinine, range 0.002–1.78). The highest excretion was 16.5 nmol/mmol creatinine, and the maximum 24-hour urine volume was 495 nmol (56 μg). The plasma bufotenine concentrations required to achieve these excretion levels are not far from the concentrations that induce psychiatric symptoms in humans. |
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| Toxicity/Toxicokinetics |
Interactions
Oral administration of two non-selective 5-HT uptake inhibitors and nine selective 5-HT uptake inhibitors one hour before subcutaneous injection of 100 mg/kg niramide in mice enhanced niramide-induced hyperkinesis, while two norepinephrine (NA) uptake inhibitors had no effect on the niramide response. Paroxetine was the most potent niramide enhancer; a dose of 0.012 mg/kg increased the motor response by 100%. Pre-subcutaneous injection of the 5-HT2 antagonist ritanserin at doses of 1 mg/kg and 10 mg/kg reduced the niramide-induced hyperkinesis induced by subcutaneous injection of 200 mg/kg niramide, but the 5-HT1 antagonist levopranolol administered in a similar manner had no effect. Subcutaneous injection of 100 mg/kg niramide into mice treated with paroxetine and lithium for 4 weeks enhanced niramide-induced hyperkinesis. Niramitide was found to have a significant synergistic effect when administered daily with paroxetine and lithium to achieve therapeutic plasma or serum concentrations. Non-human toxicity values Oral LD50 in mice: 590 mg/kg /from table/ Intravenous LD50 in mice: 120 mg/kg /from table/ Intraperitoneal LD50 in mice: 200 mg/kg /from table/ Intraperitoneal LD50 in rabbits: >150 mg/kg /from table/ For more non-human toxicity values (complete data) for niramitide (out of 6), please visit the HSDB record page. |
| Additional Infomation |
3-[[oxo(pyridin-4-yl)methyl]hydrazine]-N-(benzyl)propionamide is an organic oxygen and organic nitrogen compound. It is functionally associated with β-amino acids. Due to interactions with tyrosine-containing foods, this drug was withdrawn from the Canadian, American, and British markets in 1963. It is a monoamine oxidase inhibitor used as an antidepressant. Mechanism of Action: Niramitol is one of the earliest monoamine oxidase inhibitor (MAOI) antidepressants. It is chemically related to isopropylhydrazine, another MAOI derived from isonicotinic acid. //
Time- and dose-response analyses were performed to investigate the effects of substituted hydrazine monoamine oxidase (MAO) inhibitors isoprozid and niramide on MAO-A and MAO-B activities; the levels of γ-aminobutyric acid (GABA), alanine (ALA), and neurotransmitters dopamine, norepinephrine, and serotonin and their acidic metabolites were measured; and the activities of GABA transaminase and ALA transaminase were also measured. The results showed that these drugs are relatively potent MAO inhibitors, but unlike the unsubstituted hydrazine MAO inhibitor phenelzine, they do not increase the levels of GABA and ALA in the brain. These experiments demonstrate that the free hydrazine group is essential for the significant effects of monoamine oxidase inhibitors (MAO inhibitors) on γ-aminobutyric acid (GABA) and α-linolenic acid (ALA). Therapeutic Use A double-blind, controlled study of 30 hospitalized patients with endogenous depression evaluated the antidepressant effect of niramite plus L-5-hydroxytryptophan and compared it with a control group receiving niramite alone (plus placebo). Patients receiving niramite plus L-5-hydroxytryptophan recovered better than those receiving niramite alone. Niramite plus L-5-hydroxytryptophan had a faster onset of action. Except for orthostatic hypotension, there were no significant differences in side effects; the incidence of orthostatic hypotension was lower in patients receiving niramite plus L-5-hydroxytryptophan. /Previous Uses/ |
| Molecular Formula |
C16H18N4O2
|
|---|---|
| Molecular Weight |
298.34000
|
| Exact Mass |
298.143
|
| CAS # |
51-12-7
|
| PubChem CID |
4472
|
| Appearance |
White to off-white solid powder
|
| Density |
1.203g/cm3
|
| Boiling Point |
538.1ºC at 760mmHg
|
| Melting Point |
152-154ºC(lit.)
|
| Flash Point |
279.2ºC
|
| Index of Refraction |
1.589
|
| LogP |
2.195
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
22
|
| Complexity |
350
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
NOIIUHRQUVNIDD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H18N4O2/c21-15(18-12-13-4-2-1-3-5-13)8-11-19-20-16(22)14-6-9-17-10-7-14/h1-7,9-10,19H,8,11-12H2,(H,18,21)(H,20,22)
|
| Chemical Name |
N-benzyl-3-[2-(pyridine-4-carbonyl)hydrazinyl]propanamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~335.19 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3519 mL | 16.7594 mL | 33.5188 mL | |
| 5 mM | 0.6704 mL | 3.3519 mL | 6.7038 mL | |
| 10 mM | 0.3352 mL | 1.6759 mL | 3.3519 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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