Cyclobenzaprine
Cyclobenzaprine (MK130) is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Cyclobenzaprine also possesses antiparasitic activity. Cyclobenzaprine holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases.
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- CAS No.: 303-53-7
- Formule: C20H21N
- Masse moléculaire:275.39
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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5-HT2 Receptor |
Cyclobenzaprine (0-50 μM, 72 h) demonstrates a concentration-dependent activity in Leishmania infantum promastigotes growth, with an IC50 value of 14.5 μM[4]. Cyclobenzaprine (0-50 μM, 72 h) reduces the number of intracellular amastigotes in Leishmania infantum-infected macrophages, with an IC50 value of 12.6 μM[4]. Cyclobenzaprine (0-50 μM, 6 h) induces oxidative stress in Leishmania infantum in a concentration- and time-dependent manner[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Leishmania infantum-infected BALB/c mice model[3]
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Dosage:12.32, 24.64 and 49.28 mg/kg
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Administration:Oral gavage (i.g.), once daily for 5 days
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Result:Was effective in reducing the parasite load by 40.4% and 66.7% in spleen at 24.64 and 49.28 mg/kg, respectively and by 85.6% and 89.3% in liver at 24.64 and 49.28 mg/kg.
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Animal Model:Spinalized Male Wistar rats; Non-spinalized/Intact Male Wistar rats [5]
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Dosage:0.3, 1.0, 3.0 mg/kg
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Administration:Intravenous injection (i.v.), single dose
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Result:Dose-dependently reduced the monosynaptic reflex amplitude in non-spinalized rats, whereas it did not change the monosynaptic reflex amplitude in spinalized rats. Significantly inhibited the effect of the 5-HT2 receptor agonist DOI at the dose of 1 mg/kg, which had significantly increased the monosynaptic reflex in spinalized rats at 5 minutes.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 303-53-7
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Masse moléculaire 275.39
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Formule C20H21N
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SMILES
CN(C)CC/C=C1C2=C(C=CC=C2)C=CC3=C/1C=CC=C3
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Synonyms
MK130
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Khan I, et al. 2023 Aug 28. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2025 Jan–. [Content Brief]
[2]. Honda, M., T. Nishida, and H. Ono, Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol, 2003. 458(1-2): p. 91-9. [Content Brief]
[3]. Borenstein D G & Korn S. Efficacy of a low-dose regimen of cyclobenzaprine hydrochloride in acute skeletal muscle spasm: results of two placebo-controlled trials[J]. Clinical therapeutics, 2003, 25(4): 1056-1073. [Content Brief]
[4]. Share N N, et al. Cyclobenzaprine: a novel centrally acting skeletal muscle relaxant[J]. Neuropharmacology, 1975, 14(9): 675-684. [Content Brief]
[5]. Cunha-Júnior EF, et al. Cyclobenzaprine Raises ROS Levels in Leishmania infantum and Reduces Parasite Burden in Infected Mice. PLoS Negl Trop Dis. 2017 Jan 3;11(1):e0005281. [Content Brief]
[6]. Kobayashi, H., Y. Hasegawa, and H. Ono, Cyclobenzaprine, a centrally acting muscle relaxant, acts on descending serotonergic systems. Eur J Pharmacol, 1996. 311(1): p. 29-35. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cyclobenzaprine Related Classifications
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