| CAS NO: | 6202-23-9 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 1g | 电议 |
| 5g | 电议 |
| Cas No. | 6202-23-9 |
| 别名 | 盐酸环苯扎林; MK130 hydrochloride |
| 化学名 | 3-(5H-dibenzo[a,d][7]annulen-5-ylidene)-N,N-dimethylpropan-1-amine hydrochloride |
| Canonical SMILES | CN(CC/C=C1C2=CC=CC=C2C=CC3=CC=CC=C3\1)C.Cl |
| 分子式 | C20H22ClN |
| 分子量 | 311.85 |
| 溶解度 | ≥ 15.59mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Cyclobenzaprine is a 5-HT2 receptor antagonist and inhibitor, in some article, cyclobenzaprine hydrochloride was used as the compound to research in cyclobenzaprine. Cyclobenzaprine inhibits the enhancement of the monosynaptic reflex (MSR) induced by 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI). Cyclobenzaprine strongly binds to 5-HT2 receptors with a Ki value of 62 nM. Cyclobenzaprine binds to 5-HT1 receptor with a Ki value of 2900 nM [1] [2]. 5-HT2 receptors are G-protein coupled. They comprise three subtypes that are related in their amino acid sequence, molecular structure and signaling properties: 5-HT2A, 5-HT2B and 5-HT2C receptors. With widespread distribution in the central nervous system, 5-HT2A and 5-HT2C receptors function there. In the central nervous system, 5-HT2B receptors are restrictedly expressed [3]. In 16 of 21 spontaneously active neurons, the administration of cyclobenzaprine at 1 mg/kg decreased the discharge rate of neurons, while two neurons showed no response and three neurons demonstrated an increased rate. The decrease amount varied widely but was always ≥ 25%. In three cases, the decrease amounts were 100%. In all cases, the cell response to cyclobenzaprine followed the MSR response very closely in time [2]. After DOI treatment in rats, treatment with cyclobenzaprine increased the mono- and polysynaptic reflex amplitudes to about 150% of control level. In intact (nonspinalized) rats, the amplitude of mono- and polysynaptic reflex potentials were significantly reduced by cyclobenzaprine hydrochloride (300 μg/kg, i.v.). Within 15 min after the administration of cyclobenzaprine, the maximum effect was obtained, and this effect persisted for over 60 min. The mono- and polysynaptic reflex amplitudes were inhibited by cyclobenzaprine by about 20% and 40%, respectively. In intact rats, the depression of the mono- and polysynaptic reflex potentials induced by cyclobenzaprine hydrochloride (300 μg/kg, i.v.) was significantly inhibited by 5-HT depletion. 15 min after the administration of cyclobenzaprine in control rats, the mono- and polysynaptic reflex amplitudes were reduced to about 40–50% of the preadministration value [1]. References: |
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