Cyclobenzaprine HCl5-HT2 receptor antagonist CAS# 6202-23-9 |
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| Cas No. | 6202-23-9 | SDF | Download SDF |
| PubChem ID | 22576 | Appearance | Powder |
| Formula | C20H22ClN | M.Wt | 311.85 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | H2O : ≥ 100 mg/mL (320.67 mM) DMSO : 50 mg/mL (160.33 mM; Need ultrasonic) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 3-(dibenzo[1,2-a:1',2'-e][7]annulen-11-ylidene)-N,N-dimethylpropan-1-amine;hydrochloride | ||
| SMILES | CN(C)CCC=C1C2=CC=CC=C2C=CC3=CC=CC=C31.Cl | ||
| Standard InChIKey | VXEAYBOGHINOKW-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C20H21N.ClH/c1-21(2)15-7-12-20-18-10-5-3-8-16(18)13-14-17-9-4-6-11-19(17)20;/h3-6,8-14H,7,15H2,1-2H3;1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
Cyclobenzaprine HCl Dilution Calculator
Cyclobenzaprine HCl Molarity Calculator
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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:
[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.
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Development and Optimization of Controlled Porosity Osmotic Tablets of Lamotrigine Solid Dispersion.[Pubmed:27712567]
Recent Pat Drug Deliv Formul. 2016;10(3):222-234.
BACKGROUND: The purpose of this study was to investigate the application of a controlled porosity osmotic tablet (CPOT) utilizing solid dispersion (SD) of poorly soluble drug. The patents on Cyclobenzaprine HCl (US4968507 A) and Venlafaxine salts (EP 2085078 A1) helped in the selection of drug and polymers. METHOD: The SDs having different ratio of drug to carrier (PVP K 30) were prepared by kneading method and optimized. Effect of three independent variables, total amount of osmogen (mannitol& potassium chloride), total amount of polymer (polyethylene oxide WSR 301, hydroxy propyl methyl cellulose K100 M) and polymer1: polymer 2 ratio were investigated using Box Behnken design. Core and coated tablets were evaluated for various parameters. In-vitro drug release profiles of CPOT tablets were compared with reference product Diffcore tablet, Lamictal XR (GlaxoSmith Kline Inc., USA). RESULTS: All formulations showed acceptable parameters. Drug release from CPOT was determined as complete, zero order and pH-independent within the physiological pH range of the GI tract. Drug release was directly proportional to initial level of polymers and osmogens. CONCLUSION: The present results confirmed that prepared LTG SD serves as solubility modulator. Further, CPOT of LTG based on SD proved to be successful in delivering the drug in a controlled manner ensuring the once daily dosing for the treatment of convulsive disorders.
