生物活性

• 描述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^[3]. The prophylactic intake of tolperisone hydrochloride provides no relief to pain in course of post-exercise muscle soreness but results in reduction in isometric force^[4]. Tolperisone inhibited the spontaneous movement and methamphetamine-induced hyperactivity in mice and the ED50 was approx. 50 mg/kg, s.c. Tolperisone inhibited convulsions induced by pentylenetetrazol, nicotine and maximum electric shock, but did not affect convulsions induced by strychnine and picrotoxin. Tolperisone induced muscle relaxation in mice and rats in several pharmacological tests, but did not affect neuro-muscular transmission. Tolperisone reduced decerebrated rigidity in cats with i.v. administration of 5 approximately 10 mg/kg and intraduodenal administration of 50 approximately 100 mg/kg^[5]. Moreover, Tolperisone-HCl (5-10 mg/kg, i.v.) and baclofen (1-3 mg/kg, i.v.) decreased the number of post-rotatory nystagmus beats dose-dependently^[6]. Tolperisone (2.5-10 mg/kg) dose-dependently inhibited both ventral root reflexes and the dorsal root reflex. It slightly prolonged the dorsal root potential without affecting the amplitude^[7].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  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 Collapse <<
  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 Collapse <<
  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 Collapse <<

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• 参考文献

• [1] Hofer D, Lohberger B, et al. A comparative study of the action of tolperisone on seven different voltage dependent sodium channel isoforms. Eur J Pharmacol. 2006 May 24;538(1-3):5-14.

  [2] Pratzel HG, Alken RG, et al. Efficacy and tolerance of repeated oral doses of tolperisone hydrochloride in the treatment of painful reflex muscle spasm: results of a prospective placebo-controlled double-blind trial. Pain. 1996 Oct;67(2-3):417-25.

  [3] Rabbani G, Lee EJ, Ahmad K, Baig MH, Choi I. Binding of Tolperisone Hydrochloride with Human Serum Albumin: Effects on the Conformation, Thermodynamics, and Activity of HSA. Mol Pharm. 2018 Apr 2;15(4):1445-1456

  [4] Bajaj P, Arendt-Nielsen L, Madeleine P, Svensson P. Prophylactic tolperisone for post-exercise muscle soreness causes reduced isometric force--a double-blind randomized crossover control study. Eur J Pain. 2003;7(5):407-18

  [5] Fujii Y, Ishii Y, Suzuki T, Murayama S. [Neuropharmacological studies on tolperisone hydrochloride (author's transl)]. Nihon Yakurigaku Zasshi. 1979 Oct;75(7):655-68. Japanese

  [6] Ishikawa M, Nago M, Miyazaki H, Fukuda H. Effects of centrally acting muscle relaxants on post-rotatory nystagmus in the rabbit. Gen Pharmacol. 1989;20(1):47-51

  [7] Farkas S, Tarnawa I, Berzsenyi P. Effects of some centrally acting muscle relaxants on spinal root potentials: a comparative study. Neuropharmacology. 1989 Feb;28(2):161-73

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