Orphenadrine CitrateAntiparkinsonian and analgesic drug CAS# 4682-36-4 |
Quality Control & MSDS
3D structure
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Number of papers citing our products
| Cas No. | 4682-36-4 | SDF | Download SDF |
| PubChem ID | 83823 | Appearance | Powder |
| Formula | C24H31NO8 | M.Wt | 461.5 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 100 mg/mL (216.68 mM; Need ultrasonic) H2O : 10 mg/mL (21.67 mM; Need ultrasonic) | ||
| Chemical Name | N,N-dimethyl-2-[(2-methylphenyl)-phenylmethoxy]ethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid | ||
| SMILES | CC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C.C(C(=O)O)C(CC(=O)O)(C(=O)O)O | ||
| Standard InChIKey | MMMNTDFSPSQXJP-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C18H23NO.C6H8O7/c1-15-9-7-8-12-17(15)18(20-14-13-19(2)3)16-10-5-4-6-11-16;7-3(8)1-6(13,5(11)12)2-4(9)10/h4-12,18H,13-14H2,1-3H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
Target: NMDA Receptor
Orphenadrine has been used as an antiparkinsonian, antispastic and analgesic drug. Orphenadrine inhibits [3H]MK-801 binding to the phencyclidine (PCP) binding site of the N-methyl-D-aspartate (NMDA)-receptor in homogenates of postmortem human frontal cortex with a Ki-value of 6.0 +/- 0.7 microM. The NMDA receptor antagonistic effects of orphenadrine were assessed using concentration- and patch-clamp techniques on cultured superior colliculus neurones. Orphenadrine blocked open NMDA receptor channels with fast kinetics and in a strongly voltage-dependent manner. The IC50-value against steady state currents at -70 mV was 16.2 +/- 1.6 microM (n = 6). Orphenadrine exhibited relatively fast, concentration-dependent open channel blocking kinetics (Kon 0.013 +/- 0.002 10(6) M-1S-1) whereas the offset rate was concentration-independent (Koff 0.230 +/- 0.004 S-1) [1]. Orphenadrine competitively inhibited [3H]nisoxetine binding in rat vas deferens membranes (Ki = 1.05+/-0.20 microM). It can be concluded that orphenadrine, at low micromolar concentrations, interacts with the noradrenaline reuptake system inhibiting its functionality and thus potentiating the effect of noradrenaline [2]. References: | |||||
Orphenadrine Citrate Dilution Calculator
Orphenadrine Citrate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.1668 mL | 10.8342 mL | 21.6685 mL | 43.3369 mL | 54.1712 mL |
| 5 mM | 0.4334 mL | 2.1668 mL | 4.3337 mL | 8.6674 mL | 10.8342 mL |
| 10 mM | 0.2167 mL | 1.0834 mL | 2.1668 mL | 4.3337 mL | 5.4171 mL |
| 50 mM | 0.0433 mL | 0.2167 mL | 0.4334 mL | 0.8667 mL | 1.0834 mL |
| 100 mM | 0.0217 mL | 0.1083 mL | 0.2167 mL | 0.4334 mL | 0.5417 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Orphenadrine has been used as an antiparkinsonian, antispastic and analgesic drug. Orphenadrine inhibits [3H]MK-801 binding to the phencyclidine (PCP) binding site of the N-methyl-D-aspartate (NMDA)-receptor in homogenates of postmortem human frontal cort
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Development of a capillary electrophoresis method for the determination of orphenadrine citrate in tablets in the presence of paracetamol.[Pubmed:23960732]
Saudi Pharm J. 2010 Oct;18(4):233-7.
A validated method using capillary electrophoresis was developed, for the determination of Orphenadrine Citrate in its tablet formulations, in the presence of paracetamol. The method employs a running buffer of 30 mM pentane sulfonate sodium, dissolved in 20 mM MOPS buffer pH 7.7. Samples were injected using hydrodynamic sample injection mode (25 mbar, for 25 s), using positive polarity of 25 kV, at a constant temperature of 30 degrees C. Samples of Orphenadrine Citrate alone or in mixture solutions with paracetamol were exposed to various degradation conditions, and were electrophoresed using the recommended condition. The method was found to be specific, linear (r (2) = 0.994), precise, accurate, and robust, with an LOQ of 0.02 mg/mL. The proposed method was successfully applied for measurement of the percentage per label of Orphenadrine Citrate in commercially available tablets.
Validated stability-indicating reversed-phase-HPLC method for simultaneous determination of orphenadrine citrate, caffeine and aspirin.[Pubmed:23124566]
Chem Pharm Bull (Tokyo). 2012;60(11):1426-36.
New, simple, rapid and precise reversed-phase high-performance liquid chromatographic method was developed for the simultaneous determination of Orphenadrine Citrate, caffeine and aspirin in presence of aspirin degradation products, Orphenadrine Citrate and caffeine process related impurities, and excipients. Good resolution and quantization were achieved on reversed-phase column [Phenomenex Luna ODS C(18) (25 cmx4.6 mm, 5 microm particles)]. Gradient elution based on; eluant [A]: 0.1% triethylamine in aqueous potassium dihydrogen phosphate buffer (50 mM; pH 3.0), while as, eluant [B]: acetonitrile, at a flow rate of 1.5 mL min(-1). UV quantitation was set at 215 nm. Linearity was exhibited for Orphenadrine Citrate, caffeine and aspirin within 0.5-150, 0.5-360 or 0.7-301 microg mL(-1) ranges, respectively. Satisfactory validation results were ascertained in terms of low limits of quantiation (6.33x10(-2)-7.94x10(-2)), mean percentage recovery (98.9-101.4%), precision (<2%) and robustness. The proposed method was proved to be specific, robust and accurate for the determination of cited drugs in pharmaceutical preparations in presence of their degradation products.
Determination of paracetamol and orphenadrine citrate in pharmaceutical tablets by modeling of spectrophotometric data using partial least-squares and artificial neural networks.[Pubmed:17917430]
Yakugaku Zasshi. 2007 Oct;127(10):1723-9.
The estimation of paracetamol and Orphenadrine Citrate in a multicomponent pharmaceutical dosage form by spectrophotometric method has been reported. Because of highly interference in the spectra and the presence of non-linearity caused by the analyte concentrations which deviate from Beer and Lambert's law, partial least-squares (PLS) and artificial neural networks (ANN) techniques were used for the calibration. A validation set of spiked samples was employed for testing the accuracy and precision of the methods. Reasonably good recoveries were obtained with PLS for paracetamol and the use of an ANN allowed the estimation of Orphenadrine Citrate, a minor component which could not be adequately modeled by PLS. Three production batches of a commercial sample were analysed, and there was statistically no significant difference (P<0.05) between the results with the proposed method and those obtain with the official comparative method.
