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盐酸托哌酮 /Tolperisone HCl {[allProObj[0].p_purity_real_show]}

货号:A396302 同义名: 托哌酮盐酸盐 / Tolperisone (hydrochloride);N-553

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

Tolperisone HCl 化学结构 CAS号:3644-61-9
Tolperisone HCl 化学结构
CAS号:3644-61-9
Tolperisone HCl 3D分子结构
CAS号:3644-61-9
Tolperisone HCl 化学结构 CAS号:3644-61-9
Tolperisone HCl 3D分子结构 CAS号:3644-61-9
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Tolperisone HCl 纯度/质量文件 产品仅供科研

货号:A396302 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Sodium Channel 其他靶点 纯度
Tolperisone HCl 99%
Lamotrigine 98%
Vinpocetine 98%
Zonisamide 98%
Dronedarone Hydrochloride 95%
Procainamide hydrochloride 99%
Bupivacaine HCl 99+%
Benzocaine 98%
Carbamazepine ++

Sodium channel, IC50: 131 μM

98%
Quinidine sulfate dihydrate 98%
Ibutilide fumarate 99%+
Dibucaine HCl 99+%
Mexiletine HCl 99%
Phenytoin 99+%
Camostat Mesylate +++

epithelial sodium channel (ENaC), IC50: 50 nM

99%+
Levobupivacaine 97+%
Oxcarbazepine +

sodium channel, IC50: 160 μM

98%
Ambroxol 98+%
Primidone 99%
Propafenone 99%
A-803467 ++++

Na(V1.8) channel, IC50: 8 nM

99%+
Rufinamide 99%
Phenytoin sodium 98%
Proparacaine Hydrochloride +

Voltage-gated sodium channel, ED50: 3.4 mM

98+%
Riluzole 97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Tolperisone HCl 生物活性

靶点
  • Sodium Channel

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].

Tolperisone HCl 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 ... 展开 >> 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 收起 <<
NCT00531466 Muscle Spasticity Phase 2 Terminated - United States, California ... 展开 >> 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 收起 <<
NCT03353922 Driving Impaired Phase 1 Completed - United States, California ... 展开 >> Collaborative Neuroscience Network Long Beach, California, United States, 92845 United States, Georgia NeuroTrials Research Atlanta, Georgia, United States, 30342 收起 <<

Tolperisone HCl 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

Tolperisone HCl 实验方案

计算器
存储液制备 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

Tolperisone HCl 技术信息

CAS号3644-61-9
分子式C16H24ClNO
分子量 281.821
别名 托哌酮盐酸盐 ;Tolperisone (hydrochloride);N-553;Tolperisone hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 105 mg/mL(372.58 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(354.84 mM),配合低频超声助溶

动物实验配方
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