| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 1g | |||
| Other Sizes |
| ln Vitro |
- 5-HT receptor binding assay: Pimethixene acts as a highly selective 5-HT₂B receptor antagonist, exhibiting high affinity for 5-HT₂B receptor with a Ki value of 0.8 nM[1]
- Receptor subtype selectivity: Pimethixene shows weak affinity for 5-HT₂C receptor (Ki = 54 nM) and negligible binding to 5-HT₂A receptor (Ki > 1000 nM), demonstrating high subtype selectivity[1] |
|---|---|
| ln Vivo |
- Guinea pig neurogenic dural plasma protein extravasation model: Intraperitoneal administration of Pimethixene (0.1, 0.3, 1 mg/kg) dose-dependently inhibits trigeminal nerve stimulation-induced dural plasma protein extravasation[1]
- Efficacy magnitude: At the dose of 1 mg/kg, Pimethixene achieves a maximum inhibition rate of approximately 80% on dural plasma protein extravasation, which is statistically significant compared to the vehicle control group[1] |
| Enzyme Assay |
- 5-HT receptor competitive binding assay: Cell membrane preparations expressing human 5-HT₂B, 5-HT₂A, and 5-HT₂C receptors are prepared separately. Membrane samples are incubated with a fixed concentration of radiolabeled 5-HT ligand and various concentrations of Pimethixene at 25°C for 90 minutes. After incubation, samples are filtered through glass fiber filters to separate bound and free radioligands, and the filters are washed with ice-cold buffer. Radioactivity is measured using a scintillation counter, and Ki values for each receptor subtype are calculated via nonlinear regression analysis of competition binding curves[1]
|
| Animal Protocol |
- Guinea pig dural plasma protein extravasation assay: Male guinea pigs are randomly divided into vehicle control group and Pimethixene treatment groups (0.1, 0.3, 1 mg/kg). Pimethixene is dissolved in an appropriate vehicle and administered via intraperitoneal injection. Thirty minutes after drug administration, trigeminal ganglion electrical stimulation is performed to induce neurogenic dural inflammation. Radiolabeled albumin is intravenously injected immediately after stimulation, and guinea pigs are sacrificed 15 minutes later. Dural tissues are isolated, and the radioactivity count in the dura is measured to quantify plasma protein extravasation. The inhibition rate is calculated by comparing with the control group[1]
|
| References | |
| Additional Infomation |
1-Methyl-4-(9-thioxanthene methylene)piperidine belongs to the thioxanthracene class of compounds.
Pyroxythiazide has been approved for use in Brazil under the trade name Muricalm. It is an anticholinergic drug used to treat bronchitis. -Pyroxythiazide (code name: BF-1) is a novel selective 5-HT₂B receptor antagonist [1] -Pyroxythiazide's inhibitory effect on neurogenic dural plasma extravasation is mediated by specific blocking of 5-HT₂B receptors [1] -Neurogenic dural plasma extravasation is a key pathological process associated with migraine, suggesting that pyroxythiazide may have potential value in treating migraine [1] |
| Molecular Formula |
C19H19NS
|
|---|---|
| Molecular Weight |
293.42600
|
| Exact Mass |
293.124
|
| CAS # |
314-03-4
|
| Related CAS # |
Pimethixene maleate;13187-06-9
|
| PubChem CID |
4822
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.192g/cm3
|
| Boiling Point |
439.7ºC at 760mmHg
|
| Flash Point |
219.7ºC
|
| Index of Refraction |
1.661
|
| LogP |
4.616
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
21
|
| Complexity |
382
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1CC/C(CC1)=C2C3=C(SC4=C\2C=CC=C4)C=CC=C3
|
| InChi Key |
NZLVRVYNQYGMAB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H19NS/c1-20-12-10-14(11-13-20)19-15-6-2-4-8-17(15)21-18-9-5-3-7-16(18)19/h2-9H,10-13H2,1H3
|
| Chemical Name |
1-methyl-4-thioxanthen-9-ylidenepiperidine
|
| 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) |
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
|
|---|---|
| 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 | 3.4080 mL | 17.0398 mL | 34.0797 mL | |
| 5 mM | 0.6816 mL | 3.4080 mL | 6.8159 mL | |
| 10 mM | 0.3408 mL | 1.7040 mL | 3.4080 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.
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