规格 | 价格 | |
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500mg | ||
1g | ||
Other Sizes |
靶点 |
Muscle relaxant
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体外研究 (In Vitro) |
吡啶醇是一种在1位上被3-羟基-3,3-二苯基丙基取代的哌替啶。它有肌肉松弛剂和抗帕金森药物的作用。它是一个叔醇和哌替啶的成员。3-哌啶醇丙酸乙酯与苯溴化镁经格氏反应可制得普立地诺。
可由1-哌啶丙酸乙酯和苯基溴化镁制备
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体内研究 (In Vivo) |
本研究采用随机、双盲、安慰剂对照的三向交叉研究,探讨了两种肌肉松弛剂(盐酸托培力松和甲磺酸普立地诺)对实验性下颌肌肉疼痛和下颌拉伸反射的影响。15名健康男性参加了三个随机的疗程,间隔至少一周。每次口服300毫克托培力松,8毫克甲磺酸普立地诺或安慰剂。给药1 h后,右咬肌内注射高渗生理盐水0.3 mL(5.8%),引起肌肉疼痛。受试者连续用电子10厘米视觉模拟量表(VAS)评定他们感知到的疼痛强度。通过标准化拉伸装置(位移1 mm,坡道时间10 ms)测量压痛阈值(PPT),并在基线前(基线)、给药后1小时(给药后)、持续实验肌肉疼痛期间(给药后疼痛)和疼痛消失后15分钟(痛后)诱发咬肌和颞肌预收缩(最大自主收缩15%)的短潜伏期反射反应。方差分析显示,与甲磺酸普立地诺(6.8 +/- 0.4 cm)和安慰剂(6.6 +/- 0.4 cm)相比,托培力松给药后VAS峰值疼痛评分(5.9 +/- 0.4 cm)显著降低(P=0.020)。与盐酸托培力松和安慰剂相比,给予甲磺酸普地诺与用药后PPTs显著降低相关(P=0.002),但与实验性颚肌疼痛无关。拉伸反射的标准化峰对峰振幅不受测试药物的显著影响(P=0.762),但在持续的实验颚肌疼痛期间,所有疗程的拉伸反射都显著促进(P=0.034)。综上所述,盐酸托培里森对实验性颚肌疼痛的感知强度有轻微但显著的降低,而目前剂量对短潜伏期颚肌拉伸反射没有影响。/盐酸托培力松和甲磺酸普立地诺/
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毒性/毒理 (Toxicokinetics/TK) |
mouse LD50 intraperitoneal 100 mg/kg
Antidote and Emergency Treatment /SRP:/ Immediate first aid: Ensure that adequate decontamination has been carried out. If patient is not breathing, start artificial respiration, preferably with a demand valve resuscitator, bag-valve-mask device, or pocket mask, as trained. Perform CPR if necessary. Immediately flush contaminated eyes with gently flowing water. Do not induce vomiting. If vomiting occurs, lean patient forward or place on the left side (head-down position, if possible) to maintain an open airway and prevent aspiration. Keep patient quiet and maintain normal body temperature. Obtain medical attention. /Poisons A and B/ Currance, P.L. Clements, B., Bronstein, A.C. (Eds).; Emergency Care For Hazardous Materials Exposure. 3Rd edition, Elsevier Mosby, St. Louis, MO 2005, p. 160 /SRP:/ Basic treatment: Establish a patent airway (oropharyngeal or nasopharyngeal airway, if needed). Suction if necessary. Watch for signs of respiratory insufficiency and assist ventilations if needed. Administer oxygen by nonrebreather mask at 10 to 15 L/min. Monitor for pulmonary edema and treat if necessary ... . Monitor for shock and treat if necessary ... . Anticipate seizures and treat if necessary ... . For eye contamination, flush eyes immediately with water. Irrigate each eye continuously with 0.9% saline (NS) during transport ... . Do not use emetics. For ingestion, rinse mouth and administer 5 mL/kg up to 200 mL of water for dilution if the patient can swallow, has a strong gag reflex, and does not drool ... . Cover skin burns with dry sterile dressings after decontamination ... . /Poisons A and B/ Currance, P.L. Clements, B., Bronstein, A.C. (Eds).; Emergency Care For Hazardous Materials Exposure. 3Rd edition, Elsevier Mosby, St. Louis, MO 2005, p. 160 /SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use proparacaine hydrochloride to assist eye irrigation ... . /Poisons A and B/ Currance, P.L. Clements, B., Bronstein, A.C. (Eds).; Emergency Care For Hazardous Materials Exposure. 3Rd edition, Elsevier Mosby, St. Louis, MO 2005, p. 160-1 Non-Human Toxicity Values LD50 MOUSE INTRAVENOUS 35 MG/KG /PRIDINOL HYDROCHLORIDE/ |
参考文献 |
Acta Crystallogr B Struct Sci Cryst Eng Mater. 2018 Jun 1;74(Pt 3):304-310.
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其他信息 |
Pridinol is a piperidine substituted at position 1 by a 3-hydroxy-3,3-diphenylpropyl group. It has a role as a muscle relaxant and an antiparkinson drug. It is a tertiary alcohol and a member of piperidines.
Therapeutic Uses /EXPL THER/ A randomized, double-blind, placebo-controlled three-way cross-over study was performed to investigate the effect of two muscle relaxants (tolperisone hydrochloride and pridinol mesilate) on experimental jaw-muscle pain and jaw-stretch reflexes. Fifteen healthy men participated in three randomized sessions separated by at least 1 week. In each session 300 mg tolperisone, 8 mg pridinol mesilate or placebo was administered orally as a single dose. One hour after drug administration 0.3 mL hypertonic saline (5.8%) was injected into the right masseter to produce muscle pain. Subjects continuously rated their perceived pain intensity on an electronic 10-cm visual analogue scale (VAS). The pressure pain threshold (PPT) was measured and short-latency reflex responses were evoked in the pre-contracted (15% maximal voluntary contraction) masseter and temporalis muscles by a standardised stretch device (1 mm displacement, 10 ms ramp time) before (baseline), 1 hr after medication (post-drug), during ongoing experimental muscle pain (pain-post-drug), and 15 min after pain had vanished (post-pain). Analysis of variance demonstrated significantly lower VAS peak pain scores (5.9 +/- 0.4 cm) after administration of tolperisone hydrochloride compared with pridinol mesilate (6.8 +/- 0.4 cm) and placebo (6.6 +/- 0.4 cm) (P=0.020). Administration of pridinol mesilate was associated with a significant decrease in PPTs compared with tolperisone hydrochloride and placebo (P=0.002) after medication, but not after experimental jaw-muscle pain. The normalized peak-to-peak amplitude of the stretch reflexes were not significantly influenced by the test medication (P=0.762), but were in all sessions significantly facilitated during ongoing experimental jaw-muscle pain (P=0.034). In conclusion, tolperisone hydrochloride provides a small, albeit significant reduction in the perceived intensity of experimental jaw-muscle pain whereas the present dose had no effect on the short-latency jaw-stretch reflex. /Tolperisone hydrochloride and pridinol mesilate/ |
分子量 |
295.4186
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精确质量 |
295.194
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元素分析 |
C, 81.31; H, 8.53; N, 4.74; O, 5.42
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CAS号 |
511-45-5
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相关CAS号 |
968-58-1 (HCl); 511-45-5;
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PubChem CID |
4904
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外观&性状 |
Crystals
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密度 |
1.079 g/cm3
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沸点 |
460.9ºC at 760 mmHg
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熔点 |
120-121 °C
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闪点 |
229.9ºC
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LogP |
3.736
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tPSA |
23.47
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氢键供体(HBD)数目 |
1
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氢键受体(HBA)数目 |
2
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可旋转键数目(RBC) |
5
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重原子数目 |
22
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分子复杂度/Complexity |
294
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定义原子立体中心数目 |
0
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SMILES |
C1=CC=C(C=C1)C(CCN2CCCCC2)(C3=CC=CC=C3)O
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InChi Key |
RQXCLMGKHJWMOA-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H25NO/c22-20(18-10-4-1-5-11-18,19-12-6-2-7-13-19)14-17-21-15-8-3-9-16-21/h1-2,4-7,10-13,22H,3,8-9,14-17H2
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化学名 |
1,1-diphenyl-3-piperidin-1-ylpropan-1-ol
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别名 |
pridinol; 511-45-5; 1,1-diphenyl-3-(piperidin-1-yl)propan-1-ol; Nonplesin; Lyseen; Parks; Parks 12; Parks 12 hommel;
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
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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溶解度 (体外实验) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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溶解度 (体内实验) |
注意: 如下所列的是一些常用的体内动物实验溶解配方,主要用于溶解难溶或不溶于水的产品(水溶度<1 mg/mL)。 建议您先取少量样品进行尝试,如该配方可行,再根据实验需求增加样品量。
注射用配方
注射用配方1: DMSO : Tween 80: Saline = 10 : 5 : 85 (如: 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *生理盐水/Saline的制备:将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中,得到澄清溶液。 注射用配方 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (如: 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如: 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液,加到 900 μL Corn oil/玉米油中, 混合均匀。 View More
注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如:100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中,得到0.5%CMC-Na澄清溶液;然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中,得到悬浮液。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3850 mL | 16.9251 mL | 33.8501 mL | |
5 mM | 0.6770 mL | 3.3850 mL | 6.7700 mL | |
10 mM | 0.3385 mL | 1.6925 mL | 3.3850 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。