Tizanidine

Tizanidine, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol) . Tizanidine primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI) [1][2][3][4].

Product Specifications

CAS Number

[51322-75-9]

UNSPSC

12352005

Hazard Statement

H302+H332-H361

Target

Adrenergic Receptor; Akt; Apoptosis; Wnt; β-catenin

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; Neuronal Signaling; PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Cancer; Endocrinology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Tizanidine.html

Purity

99.58

Solubility

DMSO : 22.22 mg/mL (ultrasonic; adjust pH to 3 with 1M HCl)

Smiles

ClC1=C(NC2=NCCN2)C3=NSN=C3C=C1

Molecular Formula

C9H8ClN5S

Molecular Weight

253.71

Precautions

P261-P264-P270-P271-P280-P304+P340-P330-P405-P501

References & Citations

[1]Kamen L, et al. A practical overview of tizanidine use for spasticity secondary to multiple sclerosis, stroke, and spinal cord injury. Curr Med Res Opin. 2008 Feb;24 (2) :425-39.|[2]Granfors, M. T., et al., (2004) . Tizanidine is mainly metabolized by cytochrome p450 1A2 in vitro. British journal of clinical pharmacology, 57 (3), 349–353. |[3]Zhao L, Zhao G, Xue Q. Tizanidine (Hydrochloride) Inhibits A549 Lung Cancer Cell Proliferation and Motility Through Regulating Nischarin. Onco Targets Ther. 2020 Jan 10;13:291-298. |[4]Rodríguez-Palma EJ, et al. Sex-dependent antiallodynic effect of α2 adrenergic receptor agonist tizanidine in rats with experimental neuropathic pain. Eur J Pharmacol. 2022 Apr 5;920:174855.