| Size | Price | |
|---|---|---|
| Other Sizes |
| ADME/Pharmacokinetics |
The therapeutic blood concentration range for lidocaine is mentioned for context, but no specific ADME parameters such as half-life, bioavailability, or volume of distribution are provided for nikethamide. [1]
|
|---|---|
| Toxicity/Toxicokinetics |
The literature does not provide specific toxicity data such as LD50 for nikethamide. However, it mentions that in forensic cases, toxic symptoms from lidocaine occur when its blood concentration reaches 6 μg/ml or above. Nikethamide is often used to rescue patients experiencing severe toxic effects from lidocaine. [1]
- Blood concentrations of nikethamide in analyzed forensic cases ranged from 1.25 to 106.8 μg/ml. In cerebrospinal fluid, concentrations ranged from 8.0 to 72.4 μg/ml. These are measured post-mortem concentrations from cases where the drug was administered for rescue purposes. [1] |
| References | |
| Additional Infomation |
Nicethamid appears as a clear, pale yellow viscous liquid or crystalline solid. It has a slightly bitter taste, followed by a mild warming sensation. (NTP, 1992)
Nicethamid is a pyridinecarboxamide compound with functions similar to nicotinamide. Nicethamid has been reported to be found in Corydalis, and relevant data exist. It is a central nervous system stimulant. It was previously used to treat barbiturate overdose, but it is now considered ineffective and potentially harmful for such purposes. (From Martindale, The Extra Pharmacopoeia, 30th edition, p. 1229) Nikethamide is a respiratory central stimulant used clinically to treat respiratory failure. It is also one of the drugs banned for athletes. [1] - In clinical practice, nikethamide is often used to rescue patients who are experiencing severe toxic effects from lidocaine, such as when the blood concentration of lidocaine reaches 6 μg/ml or above, leading to symptoms like slurred speech, confusion, jerk, and vertigo. [1] - The developed HPLC method is intended for the simultaneous determination of nikethamide and lidocaine in human blood and cerebrospinal fluid for forensic toxicological analysis. The method was successfully applied to analyze nikethamide in 10 forensic cases. [1] |
| Molecular Formula |
C10H14N2O
|
|---|---|
| Molecular Weight |
178.23
|
| Exact Mass |
178.11
|
| CAS # |
59-26-7
|
| PubChem CID |
5497
|
| Appearance |
Colorless to light yellow liquid（Density：1.06 g/cm3 ）
|
| Density |
1.0±0.1 g/cm3
|
| Boiling Point |
298.0±0.0 °C at 760 mmHg
|
| Melting Point |
23 °C(lit.)
|
| Flash Point |
141.1±20.4 °C
|
| Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
| Index of Refraction |
1.520
|
| LogP |
0.33
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
13
|
| Complexity |
166
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1=C([H])N=C([H])C([H])=C1[H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H]
|
| Synonyms |
beta-PyrimidumAnacardone Astrocar Anacordone
|
| 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) |
H2O : ≥ 50 mg/mL (~280.54 mM)
DMSO : ≥ 1 mg/mL (~5.61 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (561.07 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.6107 mL | 28.0536 mL | 56.1073 mL | |
| 5 mM | 1.1221 mL | 5.6107 mL | 11.2215 mL | |
| 10 mM | 0.5611 mL | 2.8054 mL | 5.6107 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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