Size | Price | Stock | Qty |
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100mg |
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500mg |
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1g |
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5g |
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Methocarbamol (Robaxin; AHR85; Lumirelax; AHR-85; Metocarbamolo), a carbamate analog of guaifenesin, is a potent carbonic anhydrase inhibitor (CAI) with sedative and musculoskeletal relaxant properties. It is used as a central muscle relaxant for the treatment of skeletal muscle spasms.
ln Vitro |
The decay periods of the EPCs and EPPs generated by phrenic nerve stimulation are markedly increased by methocarbamol (2 mM; for 20 min)[3]. Nav1.7 currents are unaffected by methocarbamol[3].
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ln Vivo |
The muscle relaxant activity of methocarbamol (200 mg/kg; ip) is 88.96%[3].
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Animal Protocol |
Animal/Disease Models: Mice with weight 20-30 g[3]
Doses: 200 mg/kg Route of Administration: IP; single dose Experimental Results: Had Muscle relaxant activity of 88.96%. |
References |
[1]. Bruce, R.B., L.B. Turnbull, and J.H. Newman, Metabolism of methocarbamol in the rat, dog, and human. J Pharm Sci, 1971. 60(1): p. 104-6.
[2]. Sica, D.A., et al., Pharmacokinetics and protein binding of methocarbamol in renal insufficiency and normals. Eur J Clin Pharmacol, 1990. 39(2): p. 193-4. [3]. Yaxin Zhang, et al. Methocarbamol blocks muscular Na v 1.4 channels and decreases isometric force of mouse muscles. Muscle Nerve. 2020 Oct 11. |
Molecular Formula |
C11H15NO5
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Molecular Weight |
241.24
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CAS # |
532-03-6
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Related CAS # |
Methocarbamol-d5;1189699-70-4;Methocarbamol-d3;1346600-86-9;Methocarbamol-13C,d3;2747917-88-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
OC(COC1=CC=CC=C1OC)COC(N)=O
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.5 mg/mL (14.51 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 35.0 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: ≥ 3.5 mg/mL (14.51 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 35.0 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: ≥ 3.5 mg/mL (14.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (103.63 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.1452 mL | 20.7262 mL | 41.4525 mL | |
5 mM | 0.8290 mL | 4.1452 mL | 8.2905 mL | |
10 mM | 0.4145 mL | 2.0726 mL | 4.1452 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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A, Effect of methocarbamol on amplitude of CMAP at 1 Hz. Representative recordings of CMAP of diaphragm muscle in control solution and methocarbamol (2 or 4 mM) solution. B,C, decrement of CMAP amplitude (25th/1st) after repetitive stimulation at 5 or 50 Hz in untreated and 2 mM B, or 4 mM C, methocarbamol treated muscles; note aggravated decrement when incubated with methocarbamol (*P < .05, **P < .01; unpaired two-tailed Student's t test; n = 3 recorded measurements) td> |
Effect of methocarbamol on muscular of Na+ channels recorded from HEK 293 cells. Recordings were performed in the whole cell configuration from cells stably expressing the α-subunit of the human Nav1.4. A, Exemplary current transients in response to depolarizing voltage pulses going from −85 to −10 mV for 10 ms in standard external solution (black line) and in the presence 2 mM methocarbamol (gray line). B, Time course of the methocarbamol effect. Voltage pulses as applied in A, were given every 2 s and peak current maxima plotted every 4 s. Current maxima (circles) were normalized for each cell to the means of current maxima obtained between 0 and 40 s. Then, 2 mM methocarbamol were applied. Means ± SD are given for all current maxima plotted (n = 16 cells tested) td> |
Voltage dependence of the methocarbamol block and recovery of Na+ channels from inactivation. A, Normalized and averaged current/voltages curves recorded in standard external solution (black circles) and in the presence of 2 mM methocarbamol (red triangles); current maxima plotted against the test potential. B, Voltage dependence of activation of the Na+ currents; data derived from I/V curves and Boltzmann equations fitted to the data points. C, Voltage dependence of inactivation of Nav1.4 channels before and after methocarbamol application. Average normalized current maxima are plotted against the prepulse potential. Boltzmann curves were fitted to the data points. D, Recovery of Nav1.4 channels from inactivation before and during methocarbamol application. Currents were induced by test pulses to −10 mV after an initial inactivating pulse and a re-activating prepulse to −105 mV (recovery). Current maxima were plotted against the variable prepulse duration. Data points were either fitted by an exponential curve with a single time constant (τ1,black line) or by an exponential equation with two time constants (τ1, fast and τ2 slow, red line). Mean values ± SD are given for n = 16 tested cells (standard external solution) and 12 cells (2 mM methocarbamol), respectively [Color figure can be viewed at wileyonlinelibrary.com] td> |