| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| Other Sizes |
| Targets |
Zoxazolamine targets IK(Ca) channels as an opener. It also targets the central nervous system as a centrally acting muscle relaxant. The compound decreases striatal dopamine metabolism without directly affecting dopamine synthesis, catabolism, reuptake, or release. It induces a pacemaker-like discharge pattern in dopaminergic neurons. Zoxazolamine is metabolized by an array of cytochrome P450 (CYP450) isoforms.
|
|---|---|
| ln Vitro |
In vitro, Zoxazolamine activates IK(Ca) channels. It decreases striatal dopamine metabolism. The compound induces a pacemaker-like discharge pattern in dopaminergic neurons. It acts as a centrally acting muscle relaxant by decreasing CNS interneuronal activity. Its effects on dopamine turnover and neuronal activity have been characterized in various in vitro systems.
|
| ln Vivo |
In pharmacological testing, zolazomin is frequently utilized as a practical marker of alterations in rodent cytochrome P-450 function. Based on test concentration data, the time-averaged serum clearance of zoxazomin was 7.22 ± 1.01 mL/min/kg. When zoxazomin was infused into the righting reflex (LRR) at three different rates, the concentrations of the drug in the brain and serum rose as soon as the action began. The concentration of zoxazomin in the cerebrospinal fluid (CSF) at the time of the LRR excursion is nearly identical to the starting concentration when the infusion is sustained for five minutes following the occurrence of LRR [1].
In vivo, Zoxazolamine is a centrally acting muscle relaxant that was formerly used as an antispasmodic and uricosuric agent. It decreases striatal dopamine metabolism without affecting dopamine concentrations. The compound is metabolized by CYP450 isoforms. Its muscle relaxant properties have been beneficial in treating rheumatic diseases. Recovery time from zoxazolamine-induced effects depends on CYP450 metabolism. |
| Enzyme Assay |
In vitro enzyme assays for Zoxazolamine involve measuring its metabolism by cytochrome P450 isoforms. CYP450 activity is assessed using liver microsomes or recombinant CYP450 enzymes. The compound is incubated with NADPH, and metabolite formation is measured by HPLC or LC-MS. For IK(Ca) channel studies, patch-clamp electrophysiology is used to measure channel activity. Dopamine metabolism is assessed by measuring dopamine and its metabolites.
|
| Cell Assay |
In vitro cell-based assays for Zoxazolamine are conducted in neuronal cell lines or primary neurons. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the compound at varying concentrations. Dopamine metabolism is assessed by measuring dopamine and metabolite levels. IK(Ca) channel activity is measured by patch-clamp electrophysiology. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive and negative controls.
|
| Animal Protocol |
Zoxazolamine in vivo studies are conducted in animal models for muscle relaxant and metabolic research. Animals are treated with Zoxazolamine via oral administration or injection. Muscle relaxation is assessed by measuring muscle tone and coordination. Dopamine metabolism in brain tissues is assessed by measuring dopamine and metabolite levels. For CYP450 metabolism studies, blood samples are collected for metabolite analysis. Animals are monitored for clinical signs. Studies are conducted in accordance with institutional animal care guidelines.
|
| ADME/Pharmacokinetics |
Zoxazolamine (MW 168.58 g/mol, C7H5ClN2O) is a centrally acting muscle relaxant and IK(Ca) channel opener. It appears as a white to off-white powder. The compound is soluble in DMSO and other organic solvents. It is stable under recommended storage conditions. Zoxazolamine is metabolized by CYP450 isoforms. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies.
|
| Toxicity/Toxicokinetics |
Zoxazolamine is generally well-tolerated at therapeutic doses. The compound is a centrally acting muscle relaxant with established safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
|
| References | |
| Additional Infomation |
Zoxazolamine is a benzoxazole drug with uricosuric and muscle relaxant effects. Zoxazolamine primarily exerts its muscle relaxant effect through the central nervous system, but its mechanism of action remains unclear.
Zoxazolamine (NSC 24995, Contrazole) is a centrally acting muscle relaxant and IK(Ca) channel opener. It decreases striatal dopamine metabolism without affecting dopamine concentrations and induces a pacemaker-like discharge pattern in dopaminergic neurons. The compound was formerly used as an antispasmodic and uricosuric agent. It is metabolized by CYP450 isoforms. Its molecular formula is C7H5ClN2O with a molecular weight of 168.58 g/mol.All applications are limited to non-human research use. |
| Molecular Formula |
C7H5CLN2O
|
|---|---|
| Molecular Weight |
168.5804
|
| Exact Mass |
168.009
|
| CAS # |
61-80-3
|
| PubChem CID |
6103
|
| Appearance |
Off-white to light brown solid powder
|
| Density |
1.481 g/cm3
|
| Boiling Point |
316.8ºC at 760 mmHg
|
| Melting Point |
181-184 °C(lit.)
|
| Flash Point |
145.4ºC
|
| Index of Refraction |
1.692
|
| LogP |
2.644
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
11
|
| Complexity |
155
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
YGCODSQDUUUKIV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C7H5ClN2O/c8-4-1-2-6-5(3-4)10-7(9)11-6/h1-3H,(H2,9,10)
|
| Chemical Name |
5-chloro-1,3-benzoxazol-2-amine
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~593.19 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (14.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.9319 mL | 29.6595 mL | 59.3190 mL | |
| 5 mM | 1.1864 mL | 5.9319 mL | 11.8638 mL | |
| 10 mM | 0.5932 mL | 2.9660 mL | 5.9319 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
