Tizanidine

CAS# 51322-75-9

Tizanidine

Catalog No. BCC4082----Order now to get a substantial discount!

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Number of papers citing our products

Chemical structure

Tizanidine

3D structure

Chemical Properties of Tizanidine

Cas No. 51322-75-9 SDF Download SDF
PubChem ID 5487 Appearance Powder
Formula C9H8ClN5S M.Wt 253.71
Type of Compound N/A Storage Desiccate at -20°C
Solubility >11.5mg/mL in DMSO
Chemical Name 5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-2,1,3-benzothiadiazol-4-amine
SMILES C1CN=C(N1)NC2=C(C=CC3=NSN=C32)Cl
Standard InChIKey XFYDIVBRZNQMJC-UHFFFAOYSA-N
Standard InChI InChI=1S/C9H8ClN5S/c10-5-1-2-6-8(15-16-14-6)7(5)13-9-11-3-4-12-9/h1-2H,3-4H2,(H2,11,12,13)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Tizanidine Dilution Calculator

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Tizanidine Molarity Calculator

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Preparing Stock Solutions of Tizanidine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.9415 mL 19.7075 mL 39.4151 mL 78.8302 mL 98.5377 mL
5 mM 0.7883 mL 3.9415 mL 7.883 mL 15.766 mL 19.7075 mL
10 mM 0.3942 mL 1.9708 mL 3.9415 mL 7.883 mL 9.8538 mL
50 mM 0.0788 mL 0.3942 mL 0.7883 mL 1.5766 mL 1.9708 mL
100 mM 0.0394 mL 0.1971 mL 0.3942 mL 0.7883 mL 0.9854 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Tizanidine

Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.

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References on Tizanidine

Low doses of tizanidine synergize the anti-nociceptive and anti-inflammatory effects of ketorolac or naproxen while reducing of side effects.[Pubmed:28315341]

Eur J Pharmacol. 2017 Jun 15;805:51-57.

The aim of the present study was to determine whether Tizanidine, an alpha2-adrenoceptor agonist, is able to increase the anti-inflammatory and anti-nociceptive effects of naproxen and ketorolac with a low incidence of gastric injury and spontaneous activity in rats. The anti-inflammatory effect was assayed in a carrageenan test, and oral administration of Tizanidine (ED40 =0.94+/-0.2mg/kg), naproxen (ED40=3.18+/-0.4mg/kg), and ketorolac (ED40=16.4+/-1.9mg/kg) showed a dose-dependent effect on inflammation. The anti-nociceptive effect was assayed in the formalin test, and administration of Tizanidine (ED40=0.39+/-0.06mg/kg, p.o.), naproxen (ED40=33.9+/-3.9mg/kg, p.o.) or ketorolac (ED40=6.49+/-1mg/kg, p.o.) each showed a dose-dependent anti-nociceptive effect. The effects of combinations of Tizanidine/naproxen and Tizanidine/ketorolac were determined considering their ED40 at a rate of 1:1. Additionally, the Tizanidine/naproxen and Tizanidine/ketorolac combinations showed anti-inflammatory and anti-nociceptive effects. The Tizanidine/ketorolac combination was more potent than Tizanidine/naproxen, in both inflammatory (interaction index=0.03 Tizanidine/ketorolac and 0.07 Tizanidine/naproxen) and nociceptive (interaction index=0.005 Tizanidine/ketorolac and 0.01 Tizanidine/naproxen) processes. In both cases, Tizanidine improved naproxen and ketorolac gastrointestinal tolerability by 50%. Furthermore, co-administration of Tizanidine with naproxen or ketorolac did not modify the spontaneous activity in the same way as individual Tizanidine administration. Considering that Tizanidine increases the anti-inflammatory and anti-nociceptive effects of naproxen or ketorolac, with an increase in gastric tolerability, Tizanidine could provide therapeutic advantages in the clinical treatment of inflammation and pain.

Nanotransfersomes-loaded thermosensitive in situ gel as a rectal delivery system of tizanidine HCl: preparation, in vitro and in vivo performance.[Pubmed:28156169]

Drug Deliv. 2017 Nov;24(1):252-260.

The purpose of the current study was to develop Tizanidine HCl (TIZ; a myotonolytic agent used for treatment of spasticity) loaded nanotransfersomes intended for rectal administration, aiming to bypass the hepatic first-pass metabolism. TIZ-loaded nanotransfersomes were prepared by thin-film hydration method followed by characterization for various parameters including entrapment efficiency, vesicle diameter, in vitro release and ex vivo permeation studies. Transfersomal formulation composed of phosphatidylcholine and Tween 80 at a weight ratio of (85:15) gave a satisfactory results. It exhibited encapsulation efficiency of 52.39%, mean diameter of 150.33 nm, controlled drug release over 8 h and good permeation characteristics. Optimum formula was then incorporated into Pluronic-based thermoreversible gel using hydroxypropyl methylcellulose (HPMC) as a mucoadhesive polymer. Pharmacokinetic study was performed by rectal administration of transfersomes-loaded in situ gel to rabbits and compared with oral drug solution and rectal TIZ in situ gel. The pharmacokinetic study revealed that the transfersomal formulation successively enhanced the bioavailability of TIZ by about 2.18-fold and increased t1/2 to about 10 h as compared to oral solution. It can be concluded that encapsulation of TIZ into nanotransfersomes can achieve a dual purpose of prolonged TIZ release and enhanced bioavailability and so may be considered as a promising drug delivery system for the treatment of spasticity.

Description

Tizanidine is an α2-adrenergic receptor agonist and inhibits neurotransmitter release from CNS noradrenergic neurons.

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