Cyclobenzaprine HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Cyclobenzaprine 是5-HT2受体的拮抗剂和抑制剂,Cyclobenzaprine HCl被用来研究cyclobenzaprine化合物的功能。Cyclobenzaprine抑制1-(2,5-二甲氧基-4-碘苯基)-2-氨基丙烷(DOI)引起的突触反射(MSR)增强。Cyclobenzaprine与5-HT2受体强烈结合,Ki值为62 nM。Cyclobenzaprine与5-HT1受体结合,Ki值为2900 nM [1,2]。
5-HT2受体是G-蛋白偶联受体,包括了三个亚型,根据氨基酸序列的相关性、分子结构和信号特性分为5-HT2A、5-HT2B和5-HT2C受体。5-HT2A和5-HT 2C受体在中枢神经系统中广泛分布并发挥功能。在中枢神经系统中,5-HT2B受体的表达有限[3]。
测定21个自发活跃的神经元中cyclobenzaprine 的效果,1 mg/kg的cyclobenzaprine 降低了其中16个神经元的放电率,两个神经元毫无反应,三个神经元放电率增加。其中放电率的减少量差别很大,但始终大于等于25%。在三种情况下,减少的量为100%。在所有的情况下,MSR应答后cyclobenzaprine 引发的细胞反应在时间上十分密切[2]。
DOI处理大鼠后,与对照组相比,cyclobenzaprine 使单个和多个突触反射振幅增加约150%。在完整的大鼠中,静脉注射300 μg/kg的Cyclobenzaprine HCl显著降低了单个和多个突触反射电位的振幅。在Cyclobenzaprine 给药15分钟后,获得最大的效果,这种效果持续了60分钟。Cyclobenzaprine 分别抑制20%和40%单个和多个突触反射振幅。在完整大鼠中,降解5-HT显著抑制了静脉注射300 μg/kg的Cyclobenzaprine HCl所诱发的单个和多个突触反射电位的下降。在对照大鼠中,在Cyclobenzaprine 给药15分钟后,单个和多个突触反射的振幅减少到给药之前的40-50%[1]。
参考文献:
[1]. Honda M, Nishida T, Ono H. Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT2 receptors. European journal of pharmacology, 2003, 458(1): 91-99.
[2]. Barnes C D, Fung S J, Gintautas J. Brainstem noradrenergic system depression by cyclobenzaprine. Neuropharmacology, 1980, 19(2): 221-224.[3]. Leysen J E. 5-HT2 receptors. Current Drug Targets-CNS & Neurological Disorders, 2004, 3(1): 11-26.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 311.85 |
Cas No. | 6202-23-9 |
Formula | C20H22ClN |
Solubility | ≥15.59 mg/mL in DMSO; ≥5.32 mg/mL in EtOH; ≥54.3 mg/mL in H2O |
Chemical Name | 3-(5H-dibenzo[a,d][7]annulen-5-ylidene)-N,N-dimethylpropan-1-amine hydrochloride |
SDF | Download SDF |
Canonical SMILES | CN(CC/C=C1C2=CC=CC=C2C=CC3=CC=CC=C3\1)C.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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