51322-75-9
51322-75-9
Chemical Structure
Tizanidine
- CAS No.: 51322-75-9
- Formula:C9H8ClN5S
- Molecular Weight:253.71
IUPAC Name: 5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)benzo[c][1,2,5]thiadiazol-4-amine
InChIKey: XFYDIVBRZNQMJC-UHFFFAOYSA-N
SMILES: ClC1=C(NC2=NCCN2)C3=NSN=C3C=C1
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Tizanidine | 99.58% | 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). | ||||||||||||||||||||
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Tizanidine (Standard) | ≥98% | Tizanidine (Standard) is the analytical standard of Tizanidine (HY-B0194). This product is intended for research and analytical applications. 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). | ||||||||||||||||||||
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p-Iodoclonidine hydrochloride | 99.61% | p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM. | ||||||||||||||||||||
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UK 14819 | UK 14819 (5-Desbromo, 5-chloro brimonidine) is an α2-adrenoceptor agonist. UK 14819 inhibits stimulation-induced contractions of rabbit distal colon with an IC50 of 6.66 nM. | |||||||||||||||||||||
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Apraclonidine hydrochloride (Standard) | ≥98% | Apraclonidine (hydrochloride) (Standard) is the analytical standard of Apraclonidine (hydrochloride). This product is intended for research and analytical applications. Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution and has the ability to elevate the eye lid. | ||||||||||||||||||||
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Apraclonidine dihydrochloride | Apraclonidine (ALO 2145) dihydrochloride, a selective α2 and weak α1 receptor agonist activity, effectively low intraocular pressure (IOP) in eyes. Apraclonidine dihydrochloride is a topical ophthalmic solution. | |||||||||||||||||||||
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N-Acetyl tizanidine-d4 | N-Acetyl Tizanidine-d4 is the deuterium labeled N-Acetyl Tizanidine. | |||||||||||||||||||||
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Tizanidine hydrochloride | 99.93% | Tizanidine hydrochloride, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol). Tizanidine hydrochloride 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 hydrochloride has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine hydrochloride 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 hydrochloride can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI). | ||||||||||||||||||||
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Tizanidine-d4 hydrochloride | Tizanidine-d4 hydrochloride is deuterium labeled Tizanidine hydrochloride (HY-B0194A). Tizanidine hydrochloride, a skeletal muscle relaxant, is an orally effective central α2-adrenoceptor agonist (IC50 = 6.9 nmol). Tizanidine hydrochloride 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 hydrochloride has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine hydrochloride 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 hydrochloride can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI). | |||||||||||||||||||||
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Tizanidine-d4 | 99.93% | Tizanidine-d4 is the deuterium labeled Tizanidine (HY-B0194). 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). | ||||||||||||||||||||
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Brimonidine | 99.98% | Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist. | ||||||||||||||||||||
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Brimonidine impurity 6 | 98.96% | Brimonidine impurity 6 is an impurity of Brimonidine. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
