Cyclobenzaprine HCI

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Chemical Structure| 6202-23-9 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：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
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)
动物实验配方：
生物活性
靶点

  • 5-HT2
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

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

[1]Honda M, Nishida T, Ono H. Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol. 2003;458(1-2):91‐99

[2]Kobayashi H, Hasegawa Y, Ono H. Cyclobenzaprine, a centrally acting muscle relaxant, acts on descending serotonergic systems. Eur J Pharmacol. 1996;311(1):29‐35

[3]Long-term Use of Cyclobenzaprine for Pain: A Review of the Clinical Effectiveness. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2015