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Tizanidine

Names

[ CAS No. ]:
51322-75-9

[ Name ]:
Tizanidine

[Synonym ]:
5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine
5-chloro-N-(imidazolidin-2-ylidene)-2,1,3-benzothiadiazol-4-amine
Sirdalud
Ternelin
[14C]-Tizanidine
Tizanidina [INN-Spanish]
Zanaflex(R)
Tizanidina
MFCD00798231
Tizanidinum
Zanaflex
UNII-6AI06C00GW
5-chloro-4-(2-imidazolin-2-ylamino)-2,1,3-benzothiadiazole
Tizanidinum [INN-Latin]

Biological Activity

[Description]:

Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.Target: α2-adrenergic receptorTizanidine is a drug that is used as a muscle relaxant. It is a centrally acting α2 adrenergic agonist. It is used to treat the spasms, cramping, and tightness of muscles caused by medical problems such as multiple sclerosis, ALS, spastic diplegia, back pain, or certain other injuries to the spine or central nervous system. It is also prescribed off-label for migraine headaches, as a sleep aid, and as an anticonvulsant. It is also prescribed for some symptoms of fibromyalgia.Tizanidine has been found to be as effective as other antispasmodic drugs and has superior tolerability to that of baclofen and diazepam. Tizanidine can be very strong even at the 2 mg dose and may cause hypotension, so caution is advised when it is used in patients who have a history of orthostatic hypotension, or when switching from gel cap to tablet form and vice versa. Tizanidine can occasionally cause liver damage, generally the hepatocellular type. Clinical trials show that up to 5% of patients treated with tizanidine had elevated liver function test values, though symptoms disappeared upon withdrawal of the drug. Care should be used when first beginning treatment with tizanidine with regular liver tests for the first 6 months of treatment.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Research Areas >> Neurological Disease

[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.


[Related Small Molecules]

Isoprenaline hydrochloride | ICI 118,551 (hydrochloride) | Phenylephrine hydrochloride | Yohimbine hydrochloride | Adrenaline | Ivabradine hydrochloride | Prazosin hydrochloride | Clenbuterol hydrochloride | Phentolamine mesilate | guanfacine hydrochloride | pimozide | Sotalol hydrochloride | Carvedilol | Atenolol | Metroprolol succinate

Chemical & Physical Properties

[ Density]:
1.82 g/cm3

[ Boiling Point ]:
391.2ºC at 760 mmHg

[ Melting Point ]:
221 - 223ºC

[ Molecular Formula ]:
C9H8ClN5S

[ Molecular Weight ]:
253.71100

[ Flash Point ]:
190.4ºC

[ Exact Mass ]:
253.01900

[ PSA ]:
90.44000

[ LogP ]:
1.55320

[ Storage condition ]:
-20℃

[ Water Solubility ]:
H2O: ~29 mg/mL

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
DL0080000
CHEMICAL NAME :
2,1,3-Benzothiadiazole, 5-chloro-4-(2-imidazolin-2-ylamino)-
CAS REGISTRY NUMBER :
51322-75-9
LAST UPDATED :
199612
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C9-H8-Cl-N5-S
MOLECULAR WEIGHT :
253.73
WISWESSER LINE NOTATION :
T56 BNSNJ FM- BT5M CN BUTJ& GG

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
600 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - ataxia Skin and Appendages - hair
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,793,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
235 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay) Behavioral - ataxia Skin and Appendages - hair
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 30,793,1980

Safety Information

[ Hazard Codes ]:
Xn: Harmful;

[ Risk Phrases ]:
R22

[ Safety Phrases ]:
26-36

[ WGK Germany ]:
3

[ RTECS ]:
DK9910000

[ HS Code ]:
2934999090

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Related Compounds