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| 5g |
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Purity: ≥98%
Cyclobenzaprine HCl (also known as MK130; Flexeril), the hydrochloride salt of Cyclobenzaprine, is a potent muscle relaxant by blocking pain sensations, used as a medication for the treatment of skeletal muscle spasms and associated pain in acute musculoskeletal conditions. Cyclobenzaprine has a 62 nM Ki value and binds to 5-HT2 receptors strongly. Cyclobenzaprine has a Ki value of 2900 nM when it binds to the 5-HT1 receptor. The administration of cyclobenzaprine at a dose of 1 mg/kg resulted in a decrease in the discharge rate of 16 out of 21 spontaneously active neurons; two neurons exhibited no response, and three neurons showed an increased rate.
| Targets |
5-HT2 receptor
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
Cyclobenzaprine Hcl is a depressant of the central nervous system (CNS) and a relaxant of skeletal muscle. Target: Receptor 2A of 5-HT Cyclobenzaprine is a central nervous system (CNS) depressant as well as a skeletal muscle relaxant. Cyclobenzaprine was believed to be an agonist of alpha 2-adrenoceptors that decreased the activity of descending noradrenergic neurons, hence reducing muscle tone. The alpha 2-adrenoceptor antagonists yohimbine and idazoxan did not block the dose-dependent reduction of the monosynaptic reflex amplitude caused by cyclobenzaprine. Cyclobenzaprine-induced monosynaptic reflex depression was not attenuated by noradrenergic neuronal lesions produced by 6-hydroxydopamine. Since clobenzaprine inhibits the serotonergic, not the noradrenergic, descending systems in the spinal cord, it has a muscle-relaxing effect. It is a 5-HT2 receptor antagonist.
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| Cell Assay |
Cyclobenzaprine at a dose of 1 mg/kg reduced the discharge rate of 16 out of 21 spontaneously active neurons; two neurons did not respond, and three neurons showed an increase in the rate. Though it varied greatly, the decrease was always ≥ 25%. The decrease amounts were 100% in three cases. Under cyclobenzaprine, the cell response in every instance happened very soon after the MSR response.
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| Animal Protocol |
C57BL/6 mice (8-10 weeks old)
1 mg/kg Intraperitoneal injection, daily, for 5 days |
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| References |
| Molecular Formula |
C20H22CLN
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| Molecular Weight |
311.85
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| Exact Mass |
275.17
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| Elemental Analysis |
C, 77.03; H, 7.11; Cl, 11.37; N, 4.49
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| CAS # |
6202-23-9
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| Related CAS # |
Cyclobenzaprine-d3 hydrochloride; 1184983-42-3; Cyclobenzaprine-13C,d3 hydrochloride; 1261394-10-8; Cyclobenzaprine-d6 hydrochloride; 2748492-38-6
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| Appearance |
White to off-white crystalline powder
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| SMILES |
CN(C)CCC=C1C2=CC=CC=C2C=CC3=CC=CC=C31.Cl
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| InChi Key |
VXEAYBOGHINOKW-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
N,N-dimethyl-3-(2-tricyclo[9.4.0.03,8]pentadeca-1(15),3,5,7,9,11,13-heptaenylidene)propan-1-amine;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 110 mg/mL (352.73 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2067 mL | 16.0333 mL | 32.0667 mL | |
| 5 mM | 0.6413 mL | 3.2067 mL | 6.4133 mL | |
| 10 mM | 0.3207 mL | 1.6033 mL | 3.2067 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05683574 | Not yet recruiting | Drug: FDC of etoricoxib + cyclobenzaprine + etoricoxib placebo |
Third Molar Extraction | Eurofarma Laboratorios S.A. | June 30, 2024 | Phase 3 |
| NCT02814565 | Completed | Drug: Cyclobenzaprine HCl Drug: Placebo |
Neck Pain Back Pain Spasm |
Takeda | October 12, 2016 | Phase 3 |
| NCT00246389 | Completed | Drug: cyclobenzaprine hydrochloride | Pain Spasm |
McNeil Consumer & Specialty Pharmaceuticals, a Division of McNeil-PPC, Inc. |
July 2004 | Phase 4 |
| NCT01081990 | Completed | Drug: cyclobenzaprine | Postoperative Pain | NorthShore University HealthSystem |
April 2010 | Not Applicable |
| NCT01587274 | Completed | Drug: Naproxen Drug: Cyclobenzaprine |
Acute Low Back Pain | Montefiore Medical Center | April 2012 | Phase 4 |
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