Nikethamide
(Synonyms: 尼可刹米,N,N-Diethylnicotinamide) 目录号 : GC36742
Nikethamide (Corvin, Anacardone) is a respiratory stimulant that acts directly in the respiratory centres of brain.
Cas No.:59-26-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Nikethamide (Corvin, Anacardone) is a respiratory stimulant that acts directly in the respiratory centres of brain.
| Cas No. | 59-26-7 | SDF | |
| 别名 | 尼可刹米,N,N-Diethylnicotinamide | ||
| Canonical SMILES | O=C(C1=CC=CN=C1)N(CC)CC | ||
| 分子式 | C10H14N2O | 分子量 | 178.23 |
| 溶解度 | Water: ≥ 50 mg/mL (280.54 mM); DMSO: < 1 mg/mL (insoluble or 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 | 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 |
| 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Determination of Nikethamide by micellar electrokinetic chromatography
Biomed Chromatogr 2019 Oct;33(10):e4571.PMID:31062390DOI:10.1002/bmc.4571.
A simple, fast, sensitive and reproducible micellar electrokinetic chromatography (MEKC)-UV method for the determination of Nikethamide (NKD) in human urine and pharmaceutical formulation has been developed and validated. The method exhibits high trueness, good precision, short analysis time and low reagent consumption. NKD is an organic compound belonging to the psychoactive stimulants used as an analeptic drugs. The proposed analytical procedure consists of few steps: dilution of urine or drug in distilled water, centrifugation for 2 min (12,000g), separation by MEKC and ultraviolet-absorbance detection of NKD at 260 nm. The background electrolyte used was 0.035 mol/L pH 9 borate buffer with the addition of 0.05 mol/L sodium dodecyl sulfate and 6.5% ACN. Effective separation was achieved within 5.5 min under a voltage of 21 kV (~90 μA) using a standard fused-silica capillary (effective length 51 cm, 75 μm i.d.). The determined limit of detection for NKD in urine was 1 μmol/L (0.18 μg/mL). The calibration curve obtained for NKD in urine showed linearity in the range 4-280 μmol/L (0.71-49.90 μg/mL), with R2 0.9998. The RSD of the points of the calibration curve varied from 5.4 to 9.5%. The analytical procedure was successfully applied to analysis of pharmaceutical formulation and spiked urine samples from healthy volunteers.
Excretion and metabolism of Nikethamide in the horse
Br J Sports Med 1976 Oct;10(3):116-23.PMID:11864DOI:10.1136/bjsm.10.3.116.
It is well known that Nikethamide (N,N-diethylnicotinamide, CoramineR) is metabolized very rapidly to nicotinamide. Hence, there is difficulty in proving that Nikethamide has been used as a doping substance because nicotinamide is a normal physiological metabolite in the organism as well as a vitamin preparation. However, an intermediate metabolite (N-ethylnicotinamide) was found by us in the urine of horses treated with CoramineR. This was characterized by gas chromatography/mass spectrometry, and synthesized and identified as being N-ethylnicotinamide. The excretion and metabolism of Nikethamide after intramuscular injection in the horse was followed using quantitative gas chromatography of urine extracts over a period of several hours and the results of these experiments are reported. Changes in urinary pH had no significant effect upon either the metabolism or rate of excretion of the drug.
Determination of Nikethamide and N-ethylnicotinamide in the blood and urine of greyhounds
J Chromatogr 1979 Apr 21;172:295-302.PMID:548532DOI:10.1016/s0021-9673(00)90965-8.
Following the intramuscular administration of Nikethamide to a series of greyhounds, both plasma and urine excretion levels were obtained. A qualitative urine screening procedure for both Nikethamide and its major metabolite has been devised. The method involves solvent extraction, thin-layer and a two-system gas chromatographic system.
Simultaneous determination of Nikethamide and lidocaine in human blood and cerebrospinal fluid by high performance liquid chromatography
J Pharm Biomed Anal 2007 Apr 11;43(5):1757-62.PMID:17289323DOI:10.1016/j.jpba.2006.12.015.
Nikethamide and lidocaine are often requested to be quantified simultaneously in forensic toxicological analysis. A simple reversed-phase high performance liquid chromatography (RP-HPLC) method has been developed for their simultaneous determination in human blood and cerebrospinal fluid. The method involves simple protein precipitation sample treatment followed by quantification of analytes using HPLC at 263 nm. Analytes were separated on a 5 microm Zorbax Dikema C18 column (150 mm x 4.60 mm, i.d.) with a mobile phase of 22:78 (v/v) mixture of methanol and a diethylamine-acetic acid buffer, pH 4.0. The mean recoveries were between 69.8 and 94.4% for Nikethamide and between 78.9 and 97.2% for lidocaine. Limits of detection (LODs) for Nikethamide and lidocaine were 0.008 and 0.16 microg/ml in plasma and 0.007 and 0.14 microg/ml in cerebrospinal fluid, respectively. The mean intra-assay and inter-assay coefficients of variation (CVs) for both analytes were less than 9.2 and 10.8%, respectively. The developed method was applied to blood sample analyses in eight forensic cases, where blood concentrations of lidocaine ranged from 0.68 to 34.4 microg/ml and Nikethamide ranged from 1.25 to 106.8 microg/ml. In six cases cerebrospinal fluid analysis was requested. The values ranged from 20.3 to 185.6 microg/ml of lidocaine and 8.0 to 72.4 microg/ml of Nikethamide. The method is simple and sensitive enough to be used in toxicological analysis for simultaneous determination of Nikethamide and lidocaine in blood and cerebrospinal fluid.
Potentiation of cathinone by caffeine and Nikethamide
Pharmacol Biochem Behav 1989 Jun;33(2):299-301.PMID:2813469DOI:10.1016/0091-3057(89)90503-0.
The drug discrimination paradigm was employed to evaluate the effect of coadministration of both caffeine and Nikethamide upon the discrimination of a low dose of cathinone. In rats trained to discriminate between 0.8 mg/kg l-cathinone and its vehicle in a two-lever food-motivated operant task, 0.2 mg/kg cathinone produced 29.2% of responses on the cathinone-appropriate lever. This lever was chosen in 0 and 50% of trials with 25 mg/kg Nikethamide and 20 mg/kg caffeine, respectively. Coadministration of caffeine, Nikethamide, or caffeine plus Nikethamide with low-dose cathinone produced strong cathinone-like discriminative performance. This potentiattion of cathinone by caffeine and Nikethamide is reflective of noncontrolled drugs of abuse containing similar combinations especially for that of antiadipositum X-112, a drug containing all three agents and widely abused in Europe.