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Chemical Structure| 3644-61-9 Chemical Structure| 3644-61-9

Structure of Tolperisone HCl
CAS No.: 3644-61-9

Chemical Structure| 3644-61-9

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Tolperisone HCl is a muscle relaxant and an ion channel blocker with antispastic function.

Synonyms: Tolperisone (hydrochloride); N-553; Tolperisone hydrochloride

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Product Details of Tolperisone HCl

CAS No. :3644-61-9
Formula : C16H24ClNO
M.W : 281.82
SMILES Code : CC(CN1CCCCC1)C(C2=CC=C(C=C2)C)=O.[H]Cl
Synonyms :
Tolperisone (hydrochloride); N-553; Tolperisone hydrochloride
MDL No. :MFCD00058211
InChI Key :ZBUVYROEHQQAKL-UHFFFAOYSA-N
Pubchem ID :92965

Safety of Tolperisone HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H312-H319-H332
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • Sodium Channel

In Vitro:

Cell Line
Concentration Treated Time Description References
Rat brain synaptosomes 100 µM 20 min To evaluate the effect of tolperisone on 4-aminopyridine-induced glutamate release, results showed tolperisone significantly inhibited glutamate release Pharmaceuticals (Basel). 2023 Aug 7;16(8):1115
Rat brain synaptosomes 400, 1000 µM 20 minutes At high concentrations, inhibited potassium-induced glutamate release Int J Mol Sci. 2022 Aug 24;23(17):9564
Rat brain synaptosomes 40, 100, 400 µM 20 minutes Inhibited 4-aminopyridine-induced glutamate release in a concentration-dependent manner Int J Mol Sci. 2022 Aug 24;23(17):9564
HepG2 cells 0.0118 mg/ml 24 hours Evaluate cell viability, results showed that Tolperisone hydrochloride significantly reduced cell viability Front Pharmacol. 2019 Sep 12;10:993
HEK293 cells 0.04535 mg/ml 24 hours Evaluate cell viability, results showed that Tolperisone hydrochloride significantly reduced cell viability Front Pharmacol. 2019 Sep 12;10:993
H9c2 cells 0.004038 mg/ml 24 hours Evaluate cell viability, results showed that Tolperisone hydrochloride significantly reduced cell viability Front Pharmacol. 2019 Sep 12;10:993

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Wistar rats Partial sciatic nerve ligation (pSNL)-induced neuropathic pain model Oral 25, 50, 100 mg/kg Single dose, effects measured at 60, 120, and 180 minutes post-treatment Tolperisone exhibited acute antiallodynic effects in a neuropathic pain model and reduced elevated glutamate levels in cerebrospinal fluid Int J Mol Sci. 2022 Aug 24;23(17):9564
Rats Partial sciatic nerve ligation (pSNL)-induced neuropathic pain Oral 25, 50, 100 mg/kg Twice daily for 2 weeks To evaluate the antiallodynic effect of tolperisone on neuropathic pain, results showed chronic treatment with tolperisone significantly alleviated allodynia Pharmaceuticals (Basel). 2023 Aug 7;16(8):1115

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00532532 Muscle Spasticity Phase 2 Terminated - Czech Republic ... More >> Annes University Hospital Brno, Czech Republic, 65691 University Hospital Hradec Kralove Hradec Kralove, Czech Republic, 50005 University Hospital Plzen Plzen, Czech Republic, 30460 University Hospital Motol Praha, Czech Republic, 15006 Germany Facharzt fur Neurologie Bad Saarow, Germany, 15526 Facharztin fur Neurologie und Psychiatrie Berlin, Germany, 12555 Facharzt fur Neurologie und Psychiatrie Berlin, Germany, 13053 Private practice Berlin, Germany, D-13156 Neurological practice Bochum, Germany, 44805 Neuro-Consil GmbH Dusseldorf, Germany, 40212 X-pert-med GmbH Graefelfing, Germany, 82166 Asklepios Klinik Nord-Heidberg Hamburg, Germany, D022417 Neurological practice Koln, Germany, 50767 Russian Federation City Hospital #33 Nizhniy Novgorod, Russian Federation, 603076 Regional Clinical Hospital named Semashko Nizhniy Novgorod, Russian Federation, 603126 Institute of Human Brain St. Petersburg, Russian Federation, 194291 Leningrad Regional Clinical Hospital St. Petersburg, Russian Federation, 197376 Nikolaevskaya Hospital, Complex Rehabilitation Department St. Petersburg, Russian Federation, 198510 Serbia Clinical Center of Serbia Institute of Neurology Belgrade, Serbia, 11000 Clinical Center Nis Clinic of Neurology Nis, Serbia, 18000 Ukraine Ivano-Frankivsk Regional Clinical Hospital Ivano-Frankivsk, Ukraine, 76008 Central Clinical Hospital Ukrzalinznytsi (Dept. Neur. No. 1) Kharkiv, Ukraine, 61018 Central Clinical Hospital Ukrzalinznytsi (Dept. Neur. No. 3) Kharkiv, Ukraine, 61018 Institute of Neurology, Psychiatry and Narcology of AMS of Ukraine Kharkiv, Ukraine, 61068 Institute of Clinical Radiology of the Scientific Centre of Radiation Medicine of the AMS of Ukraine Kyiv, Ukraine, 03115 Odesa Regional Psychoneurological Dispensary Odesa, Ukraine, 65014 M.O.Semashko Republican Clinical Hospital Simferopol, Ukraine, 95017 Uzhgorod Regional Centre of Neurosurgery and Neurology Uzhorod, Ukraine, 88018 Less <<
NCT00531466 Muscle Spasticity Phase 2 Terminated - United States, California ... More >> Southern California Clinical Research, Inc. Pasadena, California, United States, 91106 United States, Florida University of Miami Miller School of Medicine Miami, Florida, United States, 33136 United States, Georgia Shepherd Center, Inc. Atlanta, Georgia, United States, 30309 United States, Maryland Internal Center for Spinal Cord Injury Kennedy Kreiger Institute Baltimore, Maryland, United States, 21205 Kernan Orthopaedics & Rehab. Hospital Baltimore, Maryland, United States, 21207 United States, New Jersey Kessler Institute for Rehab. West Orange, New Jersey, United States, 07052 United States, North Carolina Carolinas Rehabilitation Charlotte, North Carolina, United States, 28203 United States, Pennsylvania Jefferson Medical College of Thomas Jefferson University Philadelphia, Pennsylvania, United States, 19107 United States, Virginia Hunter Holmes McGuire Veterans Affairs Medical Center Richmond, Virginia, United States, 23249 Canada, Quebec Rehabilitation Hospital Health Sciences Centre Winnipeg, Quebec, Canada, R3A 1M4 Less <<
NCT03353922 Driving Impaired Phase 1 Completed - United States, California ... More >> Collaborative Neuroscience Network Long Beach, California, United States, 92845 United States, Georgia NeuroTrials Research Atlanta, Georgia, United States, 30342 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.55mL

0.71mL

0.35mL

17.74mL

3.55mL

1.77mL

35.48mL

7.10mL

3.55mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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