Size | Price | |
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500mg | ||
1g | ||
Other Sizes |
ln Vitro |
Metixene, with IC50 and Ki values of 55 nM and 15 nM, respectively, has the ability to inhibit QNB's binding to muscarinic receptors [3].
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ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Absorbed in the gastrointestinal tract following oral administration, however the extent of absorption is not known. Metabolism / Metabolites Hepatic. Metabolism occurs via sulfoxydation and N-demethylation. Hepatic. Metabolism occurs via sulfoxydation and N-demethylation. |
Toxicity/Toxicokinetics |
Toxicity Summary
Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as metixene is considered to relate to competitive antagonism of acetylcholine at muscarinic receptors in the corpus striatum, which then restores the balance. |
References |
[1]. Syvälahti EK, et al. Effects of antiparkinsonian drugs on muscarinic receptor binding in rat brain, heart and lung. Pharmacol Toxicol. 1988 Feb;62(2):90-4.
[2]. J. Hagenah, et al. Exogenous levodopa is not toxic to elderly subjects with non-parkinsonian movement disorders: further clinical evidence. , 106(3-4), 301–307. doi:10.1007/s007020050159 [3]. S L Levin, et al. Dualism in the effect of cholinolytics upon the human parotid gland deprived of parasympathetic control. Int J Clin Pharmacol Res. 1986;6(5):429-39. |
Additional Infomation |
Metixene is a member of thioxanthenes and a member of piperidines. It has a role as an antiparkinson drug, a muscarinic antagonist and a histamine antagonist.
Metixene (or methixene) is a anticholinergic used as an antiparkinsonian agent. Metixene is only found in individuals that have used or taken this drug. It is a anticholinergic used as an anti-parkinson drug. Drug Indication Used for the symptomatic treatment of parkinsonism. Mechanism of Action Parkinsonism is thought to result from an imbalance between the excitatory (cholinergic) and inhibitory (dopaminergic) systems in the corpus striatum. The mechanism of action of centrally active anticholinergic drugs such as metixene is considered to relate to competitive antagonism of acetylcholine at muscarinic receptors in the corpus striatum, which then restores the balance. Pharmacodynamics Metixene is a tertiary antimuscarinic with actions similar to those of atropine; it also has antihistaminic and direct antispasmodic properties. It is used for the symptomatic treatment of parkinsonism, including the alleviation of the extrapyramidal syndrome induced by other drugs such as phenothiazines, but, like other antimuscarinics, it is of no value against tardive dyskinesias. Metixene has been discontinued. |
Molecular Formula |
C20H23NS
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Molecular Weight |
309.46832
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Exact Mass |
309.155
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CAS # |
4969-02-2
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Related CAS # |
Metixene hydrochloride hydrate;7081-40-5;Metixene hydrochloride;1553-34-0
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PubChem CID |
4167
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Appearance |
Typically exists as solid at room temperature
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Boiling Point |
bp0.07 171-175°
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Melting Point |
< 25 °C
< 25 °C |
LogP |
4.952
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Hydrogen Bond Donor Count |
0
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Hydrogen Bond Acceptor Count |
2
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Rotatable Bond Count |
2
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Heavy Atom Count |
22
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Complexity |
349
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Defined Atom Stereocenter Count |
0
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SMILES |
CN1CCCC(CC2C3=CC=CC=C3SC3=CC=CC=C23)C1
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InChi Key |
MJFJKKXQDNNUJF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H23NS/c1-21-12-6-7-15(14-21)13-18-16-8-2-4-10-19(16)22-20-11-5-3-9-17(18)20/h2-5,8-11,15,18H,6-7,12-14H2,1H3
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Chemical Name |
1-methyl-3-(9H-thioxanthen-9-ylmethyl)piperidine
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HS Tariff Code |
2934.99.9001
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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)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2313 mL | 16.1567 mL | 32.3133 mL | |
5 mM | 0.6463 mL | 3.2313 mL | 6.4627 mL | |
10 mM | 0.3231 mL | 1.6157 mL | 3.2313 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.