MCE products for research use only. We do not sell to patients.

Cyclobenzaprine hydrochloride

MCE China：Cyclobenzaprine hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-B0740

CAS：6202-23-9

Synonyms：MK130 hydrochloride

Purity：99.59%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases

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, p.o., 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].

IC50 & Target：α1-adrenergic receptor 5-HT2A Receptor

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References：

[1]. 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]

[2]. 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]

[3]. Share N N, et al. Cyclobenzaprine: a novel centrally acting skeletal muscle relaxant[J]. Neuropharmacology, 1975, 14(9): 675-684.  [Content Brief]

[4]. 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]

[5]. 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]