货号:A210756 同义名: 环苯扎林盐酸盐 / MK130 hydrochloride;Cyclobenzaprine (hydrochloride) (CRM)
Cyclobenzaprine HCI是一种5-HT2受体拮抗剂,作为骨骼肌松弛剂和中枢神经系统(CNS)抑制剂,半衰期为32小时。
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | 5-HT ↓ ↑ | 5-HT1 ↓ ↑ | 5-HT2 ↓ ↑ | 5-HT3 ↓ ↑ | 5-HT5 ↓ ↑ | 5-HT6 ↓ ↑ | 5-HT7 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Desvenlafaxine |
++
5-HT, Ki: 40.2 nM |
98% | |||||||||||||||||
Lamotrigine |
+
5-HT (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM |
98% | |||||||||||||||||
Venlafaxine | ✔ | 99% | |||||||||||||||||
Fluvoxamine maleate | ✔ | 99% | |||||||||||||||||
Iloperidone | ✔ | 99% | |||||||||||||||||
Ziprasidone HCl | ✔ | 98+% | |||||||||||||||||
Atomoxetine HCI |
+
5-HT, Ki: 77 nM |
98% | |||||||||||||||||
Dapoxetine HCl | ✔ | 97% | |||||||||||||||||
Trazodone | ✔ | 98+% | |||||||||||||||||
Clomipramine HCl | ✔ | 98% | |||||||||||||||||
Mirtazapine | ✔ | 99+% | |||||||||||||||||
Escitalopram oxalate |
+++
5-HT, Ki: 0.89 nM |
97% | |||||||||||||||||
Duloxetine | ✔ | 98+% | |||||||||||||||||
Sertraline HCl |
++
5-HT, Ki: 13 nM |
98% | |||||||||||||||||
Citalopram HBr |
+++
serotonin reuptake, IC50: 1.8 nM |
98% | |||||||||||||||||
Latrepirdine 2HCl | ✔ | GluR | 99% | ||||||||||||||||
Fluoxetine HCl | ✔ | 99.5% | |||||||||||||||||
Paroxetine hydrochloride | ✔ | AChR | 99% | ||||||||||||||||
BMY 7378 |
++
5-HT1A, pIC50: 6.4 5-HT1D, pIC50: 5.9 |
+
5-HT2, pIC50: 5.5 |
97% | ||||||||||||||||
Flibanserin |
+++
5-HT1A, Ki: 1 nM |
+
5-HT2A, Ki: 49 nM |
98% | ||||||||||||||||
LY310762 |
+
5-HT1D, Ki: 249 nM |
99%+ | |||||||||||||||||
Cyclobenzaprine HCI | ✔ | 99% | |||||||||||||||||
Blonanserin |
+++
5-HT2, Ki: 3.98 nM |
99% | |||||||||||||||||
Cyproheptadine HCl |
++++
5-HT2, IC50: 0.6 nM |
99+% | |||||||||||||||||
Olanzapine | ✔ | 99+% | |||||||||||||||||
Pimavanserin hemitartrate |
+++
5-HT2A, pIC50: 8.7 |
99% | |||||||||||||||||
Ketanserin |
+++
5-HT2C (Human), Ki: 2.5 nM 5-HT2C (Rat), Ki: 50 nM |
99%+ | |||||||||||||||||
Loxapine succinate |
++
5-HT2 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM |
99% | |||||||||||||||||
Agomelatine | ✔ | 98% | |||||||||||||||||
Clozapine | ✔ | 98% | |||||||||||||||||
Amitriptyline |
+
5-HT2, Ki: 235 nM |
SERT | 99% | ||||||||||||||||
PRX-08066 maleate |
+++
5-HT2B, IC50: 3.4 nM |
98+% | |||||||||||||||||
RS-127445 |
++++
5-HT2B, pKi: 9.5 5-HT2B, pIC50: 10.4 |
99%+ | |||||||||||||||||
Sarpogrelate HCl |
++++
5-HT2C, Kd: 1.1 nM 5-HT2A, Kd: 2.1 nM |
98% | |||||||||||||||||
Tropisetron | ✔ | 99% | |||||||||||||||||
Palonosetron | ✔ | 98% | |||||||||||||||||
Ramosetron HCl |
++++
5-HT3 receptor, Ki: 0.091 nM |
98% | |||||||||||||||||
Ondansetron | ✔ | 99% | |||||||||||||||||
Granisetron | ✔ | 98% | |||||||||||||||||
Alosetron HCl | ✔ | 98% | |||||||||||||||||
Ondansetron hydrochloride dihydrate | ✔ | 98% | |||||||||||||||||
VUF10166 |
++++
5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM |
99%+ | |||||||||||||||||
Azasetron hydrochloride |
++++
5-HT3, IC50: 0.33 nM |
99% | |||||||||||||||||
Asenapine maleate |
+++
5-HT1A, pKi: 8.6 5-HT1B, pKi: 8.4 |
++++
5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46 |
+++
5-HT5A, pKi: 8.84 |
++++
5-HT6, pKi: 9.6 |
++++
5-HT7, pKi: 9.94 |
97% | |||||||||||||
Risperidone |
++
5-HT1D, Ki: 84.6 nM 5-HT1B, Ki: 14.9 nM |
++++
5-HT2C, Ki: 12 nM 5-HT2A, Ki: 61.9 nM |
+
5-HT5A, Ki: 206 nM |
++
5-HT7, Ki: 6.6 nM |
98% | ||||||||||||||
SB 271046 HCl |
+++
5-HT6, pKi: 8.92 |
99%+ | |||||||||||||||||
Intepirdine |
++++
5-HT6, pKi: 9.63 |
99%+ | |||||||||||||||||
SB-269970 HCl |
++
5-HT7, pKi: 8.3 |
98+% | |||||||||||||||||
BRL 15572 |
++
5-HT1B, pKi: 6.1 5-HT1D, pKi: 6 |
++
5-HT2B, pKi: 6.2 5-HT2A, pKi: 6.6 |
+
5-HT6, pKi: 5.9 |
+
5-HT7, pKi: 6.3 |
98% | ||||||||||||||
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。 |
靶点 |
|
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]. |
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 << |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 6202-23-9 |
分子式 | C20H22ClN |
分子量 | 311.848 |
别名 | 环苯扎林盐酸盐 ;MK130 hydrochloride;Cyclobenzaprine (hydrochloride) (CRM);MK-130;Cyclobenzaprine HCl |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Room Temperature |
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 |