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Tolperisone HCl

CAS# 3644-61-9

Tolperisone HCl

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Chemical structure

Tolperisone HCl

3D structure

Chemical Properties of Tolperisone HCl

Cas No. 3644-61-9 SDF Download SDF
PubChem ID 92965 Appearance Powder
Formula C16H24ClNO M.Wt 281.82
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 36 mg/mL (127.74 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one;hydrochloride
SMILES CC1=CC=C(C=C1)C(=O)C(C)CN2CCCCC2.Cl
Standard InChIKey ZBUVYROEHQQAKL-UHFFFAOYSA-N
Standard InChI InChI=1S/C16H23NO.ClH/c1-13-6-8-15(9-7-13)16(18)14(2)12-17-10-4-3-5-11-17;/h6-9,14H,3-5,10-12H2,1-2H3;1H
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.
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.
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.

Biological Activity of Tolperisone HCl

DescriptionTolperisone is a centrally acting muscle relaxant, is indicated for use in the treatment of pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the pyramidal tract, multiple sclerosis, myelopathy, encephalomyelitis) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.

Tolperisone HCl Dilution Calculator

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Tolperisone HCl Molarity Calculator

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Preparing Stock Solutions of Tolperisone HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.5484 mL 17.7418 mL 35.4836 mL 70.9673 mL 88.7091 mL
5 mM 0.7097 mL 3.5484 mL 7.0967 mL 14.1935 mL 17.7418 mL
10 mM 0.3548 mL 1.7742 mL 3.5484 mL 7.0967 mL 8.8709 mL
50 mM 0.071 mL 0.3548 mL 0.7097 mL 1.4193 mL 1.7742 mL
100 mM 0.0355 mL 0.1774 mL 0.3548 mL 0.7097 mL 0.8871 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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Background on Tolperisone HCl

Tolperisone HCl is an ion channel blocker and centrally-acting muscle relaxant.

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References on Tolperisone HCl

Considerable interindividual variation in the pharmacokinetics of tolperisone HCl.[Pubmed:17323790]

Int J Clin Pharmacol Ther. 2007 Feb;45(2):110-3.

OBJECTIVE: The aim of this study was to determine the pharmacokinetic profiles of oral tolperisone hydrochloride in healthy volunteers. METHODS: After the oral administration of tolperisone hydrochloride, the plasma concentrations of tolperisone were measured in 15 healthy male Korean volunteers. The tolperisone concentration was determined using high-performance liquid chromatography with a C18 reverse-phase column. RESULTS: Very large interindividual differences in the AUC and Cmax were detected after oral Tolperisone HCl. The AUC0-infinity, varied from 125.9-1,241.3 ng/ml x h, and the Cmax varied from 64.2 and 784.9 ng/ml. The tmax of tolperisone was 0.90 +/- 0.31 h and the mean half-life was 1.00 +/- 0.28 h. CONCLUSION: These results suggest that the pharmacological effect of oral Tolperisone HCl varies between individuals, and the oral Tolperisone HCl dose might need to be individualized.

Symptomatic treatment of neurolathyrism with tolperisone HCL (Mydocalm): a randomized double blind and placebo controlled drug trial.[Pubmed:9577009]

Ethiop Med J. 1997 Apr;35(2):77-91.

The efficacy and safety of oral Tolperisone HCl was evaluated in double blind, placebo-controlled, randomized trial in 72 patients with neurolathyrism in stages I, II, and III of the disease at Kolla Duba Health Centre of Dembia District of North Gondar between January and April 1995. Taken orally daily for 12 weeks, Tolperisone HCl (Mydocalm) in a dose of 150 milligrams (mgs) twice daily significantly improved subjective complaints such as muscle cramps, heaviness of the legs, startle attacks, flexor spasms and repeated falls. An overall subjective improvement was observed in 75% of the patients on Tolperisone HCl and 39% of the placebo group (P = 0.002). When objectively assessed spastic muscle tone in the abductors, stiffness of Achilles and spontaneous ankle clonus were significantly reduced in Tolperisone HCl group (P values = 0.001, 0.04, and 0.0001, respectively). Walking ability and speed of walking was also significantly improved. The drug is most effective in relieving symptoms of stage I and stage II disease. Some adverse effects like muscle pain, generalized body weakness and dizziness were recorded in patients taking the drug but all were minor and self limited, none requiring discontinuation of treatment. It is concluded that tolperisone is a well tolerated and efficacious drug for symptomatic treatment of neurolathyrism.

Description

Tolperisone hydrochloride is a centrally acting muscle relaxant, is indicated for use in the treatment of pathologically increased tone of the cross-striated muscle caused by neurological diseases (damage of the pyramidal tract, multiple sclerosis, myelopathy, encephalomyelitis) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.

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