Cyclobenzaprine  (Synonyms: MK130)

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^{[1][2][3][4][5]}.

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.

Cyclobenzaprine (starting dose of 4 mg/kg, p.o., at 60-minute intervals with incremental doses until the EMG frequency is reduced to below 10 Hz) continuously suppresses high quadriceps activity in the ischemic spinal cord rigidity cat model, with an ED₁₀₀ of 4-12 mg/kg^[3].
Cyclobenzaprine (22.8 mg/kg, p.o., single dose) prevents tonic-extensor seizures in the seizure model of male albino CF1 mice (induced by electrical stimulation or Pentylenetetrazol and Strychnine)^[3].
Cyclobenzaprine (12.32-49.28 mg/kg, i.g., once daily for 5 days) reduces the parasite load in BALB/c mice infected with Leishmania infantum^[4].
Cyclobenzaprine hydrochloride (0.3-3.0 mg/kg, i.v., single dose) blocks tonic α-motoneuronal excitation produced by serotonergic descending neurons in Spinalized Male Wistar rats^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

275.39

C₂₀H₂₁N

303-53-7

CN(C)CC/C=C1C2=C(C=CC=C2)C=CC3=C/1C=CC=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]