产品说明书
Cyclobenzaprine HCI
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同义名 : | 环苯扎林盐酸盐 ;MK130 hydrochloride;Cyclobenzaprine (hydrochloride) (CRM);MK-130;Cyclobenzaprine HCl |
| CAS号 : | 6202-23-9 | |
| 货号 : | A210756 | |
| 分子式 : | C20H22ClN | |
| 纯度 : | 99% | |
| 分子量 : | 311.848 | |
| MDL号 : | MFCD00079039 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(160.33 mM)，配合低频超声助溶，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(320.67 mM) |
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| 动物实验配方： |
| 生物活性 | |||
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| 靶点 |
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| 描述 | Cyclobenzaprine HCl, 5-HT2 receptor antagonist, is a skeletal muscle relaxant and a central nervous system (CNS) depressant. Cyclobenzaprine (HCl) was thought to be an alpha 2-adrenoceptor agonist that reduced muscle tone by decreasing the activity of descending noradrenergic neurons. Cyclobenzaprine reduced the monosynaptic reflex amplitude dose dependently and this effect was not inhibited by the alpha 2-adrenoceptor antagonists idazoxan and yohimbine. However, cyclobenzaprine inhibited monosynaptic reflex facilitation induced by (+/-)-1-(4-iodo-2,5-dimethoxyphenyl)-2-aminopropane, a 5-HT2 receptor agonist, in spinalized rats markedly, and 5-HT depletion by DL-p-chlorophenylalanine inhibited the depressive effect of cyclobenzaprine on the monosynaptic reflex[2]. The inhibitory effects of cyclobenzaprine on mono- and polysynaptic reflex potentials are due to the inhibition of descending serotonergic systems through 5-HT(2) receptors in the spinal cord[1]. Owing to its anticholinergic activity and long half-life, cyclobenzaprine is not recommended for use in the elderly[3]. | ||
| 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 |
| NCT02891759 | Breast Cancer | Phase 2 | Recruiting | April 30, 2020 | United States, Missouri ... 展开 >> Washington University School of Medicine Recruiting Saint Louis, Missouri, United States, 63110 Contact: Terence M Myckatyn, M.D. 314-996-8800 myckatyn@wustl.edu Principal Investigator: Terence M Myckatyn, M.D. Sub-Investigator: Marissa Tenenbaum, M.D. Sub-Investigator: Julie Margenthaler, M.D. Sub-Investigator: Amy Cyr, M.D. Sub-Investigator: Raj Parikh, M.D. Sub-Investigator: Elizabeth B Odom, M.D. 收起 << |
| NCT00386243 | Low Back Pain ... 展开 >> Pain Pain, Intractable 收起 << | Not Applicable | Completed | - | United States, Indiana ... 展开 >> Richard Roudebush VA Medical Center, Indianapolis Indianapolis, Indiana, United States, 46202-2884 收起 << |
| NCT02651324 | Idiopathic Scoliosis ... 展开 >> Post-operative Pain 收起 << | Phase 4 | Active, not recruiting | December 2017 | United States, New York ... 展开 >> Albany Medical Center Albany, New York, United States, 12208 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.21mL 0.64mL 0.32mL |
16.03mL 3.21mL 1.60mL |
32.07mL 6.41mL 3.21mL |
| 参考文献 |
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