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Tizanidine- Medical Intermediates

Short Description:

CAS number: 51322-75-9

Molecular formula: C9H8ClN5S

molecular weight: 253.71

Chemical structure:


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  • Product Detail

    Product Tags

    Basic Information
    Product name Tizanidine
    Grade Pharma grade
    Appearance White Powder
    Assay 99%
    Shelf life 2 years
    Packing 25kg/drum
    Condition Store at -20°C

    Outline

    Tizanidine is an imidazoline two nitrogen heterocyclic pentene derivative. The structure is similar to that of clonidine. In 1987, it was first listed in Finland as a central adrenalin α2 receptor agonist. Currently, it is used as a central muscle relaxant in clinic. It can be used to treat painful muscle spasm, such as neck waist syndrome and torticollis. It can also be used to treat postoperative pain, such as disc herniation and hip arthritis. It comes from the ankylosis of neurological disorders, such as multiple sclerosis, chronic myelopathy, cerebrovascular accident and etc.

    Function

    It is used to reduce skeletal muscle tension, muscle spasm and myotonia caused by brain and spinal cord injury, cerebral hemorrhage, encephalitis and multiple sclerosis.

    Pharmacology

    It selectively reduces the release of excitatory amino acids from interneurons and inhibits the multi synaptic mechanism related to muscle overstrain. This product does not affect the transmission of neuromuscular. It is well tolerated. It is effective for acute painful muscle spasms and chronic ankylosis originates from the spinal cord and brain. It can reduce the resistance of passive movement, reduce spasticity and clonus, and increase the intensity of voluntary movement.

    Uses

    Labeled Tizanidine, intended for use as an internal standard for the quantification of Tizanidine by GC- or LC-mass spectrometry. Tizanidine could have therapeutic use as a SARS-CoV-2 main protease inhibitor.

    Clinical Use

    Tizanidine is a centrally acting adrenergic α2 receptor agonist used to treat chronic muscle spasticity conditions, such as multiple sclerosis.

    Mechanism of action

    Tizanidine is a centrally active muscle relaxant analogue of clonidine that is approved for use in reducing spasticity associated with cerebral or spinal cord injury. Its mechanism of action for reducing spasticity suggests presynaptic inhibition of motor neurons at the α2-adrenergic receptor sites, reducing the release of excitatory amino acids and inhibiting facilitatory ceruleospinal pathways, thus resulting in a reduction in spasticity. Tizanidine only has a small fraction of the antihypertensive action of clonidine, presumably because of action at a selective subgroup of α2C-adrenoceptors, which appear to be responsible for the analgesic and antispasmodic activity of  imidazoline α2-agonists(20).


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