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Zoxazolamine

CAS# 61-80-3

Zoxazolamine

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Chemical structure

Zoxazolamine

3D structure

Chemical Properties of Zoxazolamine

Cas No. 61-80-3 SDF Download SDF
PubChem ID 6103 Appearance Powder
Formula C7H5ClN2O M.Wt 168.58
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (593.19 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 5-chloro-1,3-benzoxazol-2-amine
SMILES C1=CC2=C(C=C1Cl)N=C(O2)N
Standard InChIKey YGCODSQDUUUKIV-UHFFFAOYSA-N
Standard InChI InChI=1S/C7H5ClN2O/c8-4-1-2-6-5(3-4)10-7(9)11-6/h1-3H,(H2,9,10)
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.

Zoxazolamine Dilution Calculator

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Zoxazolamine Molarity Calculator

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Preparing Stock Solutions of Zoxazolamine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 5.9319 mL 29.6595 mL 59.319 mL 118.638 mL 148.2975 mL
5 mM 1.1864 mL 5.9319 mL 11.8638 mL 23.7276 mL 29.6595 mL
10 mM 0.5932 mL 2.966 mL 5.9319 mL 11.8638 mL 14.8298 mL
50 mM 0.1186 mL 0.5932 mL 1.1864 mL 2.3728 mL 2.966 mL
100 mM 0.0593 mL 0.2966 mL 0.5932 mL 1.1864 mL 1.483 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 Zoxazolamine

Zoxazolamine is a centrally acting myorelaxant, which is formerly used as an antispasmodic and uricosuric.

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References on Zoxazolamine

Effects of furazolidone on duration of righting reflex loss induced with hexobarbital and zoxazolamine in the rat.[Pubmed:7999888]

J Vet Med Sci. 1994 Aug;56(4):667-70.

Effects of furazolidone (FZ) on the sleeping time induced with hexobarbital (HEX) and paralysis time induced by Zoxazolamine (ZOX) were investigated by measuring the length of time required to recover from righting reflex loss in rats after oral administration of FZ at doses of 50, 100, 200 and 400 mg/kg/day for 4 successive days. Administration of 50 mg/kg to rats of both sexes induced no effect on the HEX sleeping time, but of 100 mg/kg FZ or more induced prolongation of sleeping time dose-dependently. In female rats, HEX sleeping time of the control group was twice that of the male rats, but HEX sleeping time after receiving FZ above 200 mg/kg was approximately the same as in the male rats. ZOX paralysis time exhibited no sex differences in the control rats, and it was significantly prolonged by FZ at a dose of 100 mg/kg or more. No significant differences in blood levels of HEX and ZOX at the time of recovery were found between the control and FZ treated rats, suggesting that FZ produced prolongation of the drug effects was due to the maintenance of the blood levels rather than the change in the sensitivities of rats at the receptor sites. Body weight gains were inhibited in the rats treated with FZ at doses over 100 mg/kg. Cytochrome P-450 content in hepatic microsomes in the rats which received 100 mg/kg FZ were slightly increased. It is suggested that successive oral administration of FZ to rats at high doses impaired drug clearance and this resulted in the prolongation of HEX sleeping and ZOX paralysis times.

Effects of ciprofloxacin and enrofloxacin on zoxazolamine kinetics, plasma concentration and sleeping times in mice.[Pubmed:8395094]

Toxicol Lett. 1993 Jul;69(1):1-14.

The treatment of CD1 male mice with either ciprofloxacin (CP) or enrofloxacin (EF) prior to Zoxazolamine (ZX) administration increased the mean ZX sleeping times to, respectively, 162 and 156% of the control (ZX alone). At the end of the sleeping time, the mean ZX plasma concentration in controls was 27.2 micrograms/ml and was not different in EF- or CP-treated groups (87% and 95% of controls, respectively). The animals coadministered with CP or EF and ZX eliminated the latter more slowly than the controls. The estimated zero-time drug concentration of the disposition curves of both the CP- and EF-treated groups as well as the apparent half-life of elimination and apparent overall rate of elimination of the CP-treated group were different from the control values.

Zoxazolamine-induced paralysis in two rat substrains: differences in hepatic drug metabolism.[Pubmed:10323328]

Eur J Drug Metab Pharmacokinet. 1998 Oct-Dec;23(4):461-7.

Aldehyde dehydrogenase (ALDH) is involved in the metabolism of endogenous and exogenous aldehydes originating from biogenic amines, lipids, food and drugs. Rat liver contains at least two cytosolic ALDHs that can be stimulated by inducers of drug metabolism. Phenobarbital- type inducers increase ALDH1 activity while polycyclic aromatic hydrocarbons (such as benzo[alpha]pyrene) and 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) increase ALDH3c isoenzyme activity. Two rat substrains were isolated according to a different induction of hepatic ALDH after treatment with phenobarbital (PB). Animals that responded to treatment (RR) and those that did not respond (rr) were inbred and divided into two homogenous groups. These animals constituted an ideal experimental model due to their common origin. Apart from the dramatic induction of cytosolic ALDH1 and ALDH3c, the effects of PB on pentoxy-, ethoxy- and methoxy-resorufin-O-dealkylase (P-, E-, and MROD) between the two substrains were also studied. 3-Methylcholanthrene (3MC) greatly increased ALDH3c levels in both substrains, although it was slightly more pronounced in the rr rats, in which it was assessed either as ALDH3c or as total cytosolic ALDH. A similar trend was also noted in EROD, PROD and MROD activities. Dealkylation of the methoxy group was found to be statistically different between the two substrains (rr > RR). The relevance of the biochemical findings with the in vivo hepatic capacity for drug metabolism was investigated by measuring the duration of Zoxazolamine paralysis. Both animal substrains were tested with Zoxazolamine either without pretreatment or after administration of PB or 3MC: the paralysis produced by Zoxazolamine lasted for a longer period in rr than in RR rats. After pretreatment with PB, the duration of paralysis was greatly reduced, but the differences between the two substrains remained. Pretreatment with various doses of 3MC produced differences in the duration of paralysis in RR and rr rats, although the time period was much shorter than that observed in control animals.

Synthesis and characterisation of the first transition metal complex of zoxazolamine (2-amino-5-chlorobenzoxazole): the X-ray crystal structure determination of [ZnCl2(eta 1-Nbenzoxazole-2-amino-5-chlorobenzoxazole)2].[Pubmed:15621301]

J Inorg Biochem. 2005 Feb;99(2):664-7.

The synthesis and characterisation (NMR, X-ray, elemental analysis) of the first transition metal complex of Zoxazolamine (1: 2-amino-5-chlorobenzoxazole), viz. [ZnCl(2)(1)(2)] (2) is described; complex 2 is obtained in 77% yield from the treatment of 1 with ZnCl(2) in acetone solution. The Zn compound is a mononuclear species (X-ray) with a distorted tetrahedral array of ligands around the metal centre with the title ligand bound to Zn via the benzoxazole ring N-atom. The structural properties of 2 are discussed in relation to other mononuclear Zn halide complexes.

Description

Zoxazolamine is widely used for a pharmacologic test that serves as a convenient indicator of changes in cytochrome P-450 activity in rodents.

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