Cyclobenzaprine (hydrochloride)

Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT₂ receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases^{[1][2][3][4][5]}. In Vitro: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].
In Vivo: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].