Cyclobenzaprine HCl5-HT2 receptor antagonist CAS# 6202-23-9 |
- MNS
Catalog No.:BCC3943
CAS No.:1485-00-3
- BIO 1211
Catalog No.:BCC3945
CAS No.:187735-94-0
- Cilengitide
Catalog No.:BCC3942
CAS No.:188968-51-6
- A 205804
Catalog No.:BCC3944
CAS No.:251992-66-2
- Firategrast
Catalog No.:BCC1575
CAS No.:402567-16-2
- Zaurategrast
Catalog No.:BCC2070
CAS No.:455264-31-0
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| 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. |
||
| 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. |
||
| 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
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
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.
- Bulgarsenine
Catalog No.:BCN2065
CAS No.:62018-77-3
- Helichrysetin
Catalog No.:BCN4149
CAS No.:62014-87-3
- p-Menthane-1,2,8-triol
Catalog No.:BCN4148
CAS No.:62014-81-7
- Dirithromycin
Catalog No.:BCC4656
CAS No.:62013-04-1
- CCG-63808
Catalog No.:BCC1461
CAS No.:620113-73-7
- CCG-63802
Catalog No.:BCC1460
CAS No.:620112-78-9
- Senkyunolide A
Catalog No.:BCN6351
CAS No.:62006-39-7
- 4,4'-Methylenediphenol
Catalog No.:BCN2690
CAS No.:620-92-8
- Hyoscyamine sulfate hydrate
Catalog No.:BCN2846
CAS No.:620-61-1
- Tribenzylamine
Catalog No.:BCN1817
CAS No.:620-40-6
- 5-Methyl-2-furaldehyde
Catalog No.:BCN3801
CAS No.:620-02-0
- Diphemanil Methylsulfate
Catalog No.:BCC3767
CAS No.:62-97-5
- Juncusol
Catalog No.:BCN2926
CAS No.:62023-90-9
- Ginsenoside F2
Catalog No.:BCN1245
CAS No.:62025-49-4
- Ginsenoside F3
Catalog No.:BCN1077
CAS No.:62025-50-7
- 4-(Dimethylamino)cinnamaldehyde
Catalog No.:BCN4968
CAS No.:6203-18-5
- Onitisin 2'-O-glucoside
Catalog No.:BCN4150
CAS No.:62043-53-2
- Hydroxycitric acid
Catalog No.:BCN2912
CAS No.:6205-14-7
- Nudiposide
Catalog No.:BCN7437
CAS No.:62058-46-2
- Heliotrine N-oxide
Catalog No.:BCN1983
CAS No.:6209-65-0
- 3-Nitro-L-tyrosine
Catalog No.:BCN2213
CAS No.:621-44-3
- Isovanillin
Catalog No.:BCN2502
CAS No.:621-59-0
- Scutebarbatine E
Catalog No.:BCN8396
CAS No.:910099-77-3
- Benzyl carbamate
Catalog No.:BCC8871
CAS No.:621-84-1
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.
