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盐酸环苯扎林 /Cyclobenzaprine HCI 99%

货号:A210756 同义名: 环苯扎林盐酸盐 / MK130 hydrochloride;Cyclobenzaprine (hydrochloride) (CRM) Ambeed 开学季,买赠积分,赢豪礼

Cyclobenzaprine HCl is a 5-HT2 receptor antagonist as a skeletal muscle relaxant and a central nervous system (CNS) depressant with elimination half-life of ‎32 hours.

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Cyclobenzaprine HCI 化学结构 CAS号:6202-23-9
Cyclobenzaprine HCI 化学结构
CAS号:6202-23-9
Cyclobenzaprine HCI 3D分子结构
CAS号:6202-23-9
Cyclobenzaprine HCI 化学结构 CAS号:6202-23-9
Cyclobenzaprine HCI 3D分子结构 CAS号:6202-23-9
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Cyclobenzaprine HCI 纯度/质量文件 产品仅供科研

货号:A210756 标准纯度: 99%
批次查询: 批次纯度:

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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

99%+
Venlafaxine 99%+
Fluvoxamine maleate 99%
Iloperidone 99%+
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 99%+
Trazodone 98+%
Clomipramine HCl 99%+
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

99%+
Duloxetine 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

99%+
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

99%+
Latrepirdine 2HCl GluR 99%+
Fluoxetine hydrochloride 98%
Paroxetine hydrochloride AChR 99%+
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

+

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 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

99%
Agomelatine 99%+
Clozapine 99%+
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 98%
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-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

98%
Tropisetron 99%
Palonosetron 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

99%+
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron hydrochloride dihydrate 99%+
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

98%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

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

99%+
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

99%+
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-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

+

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。

Cyclobenzaprine HCI 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].

Cyclobenzaprine HCI 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 <<

Cyclobenzaprine HCI 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

Cyclobenzaprine HCI 实验方案

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

Cyclobenzaprine HCI 技术信息

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

粉末 Inert atmosphere,Room Temperature

液体 -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
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