| Size | Price | Stock | Qty |
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| 1g |
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| Other Sizes |
| Targets |
Tetrahydropalmatine targets dopamine receptors, functioning as a dopamine receptor antagonist. It exhibits a distinct binding preference for D1 receptors over D2 receptors in vitro. The compound is also a novel and effective voltage-activated L-type calcium channel blocker. By blocking dopamine receptors and calcium channels, tetrahydropalmatine exerts its analgesic and sedative effects. Its mechanism may also involve inhibition of amygdaloid dopamine release.
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| ln Vitro |
In vitro, tetrahydropalmatine acts as a dopamine receptor antagonist with a preference for D1 receptors. It also functions as a voltage-activated L-type calcium channel blocker. These activities contribute to its analgesic and sedative properties. The compound's affinity for dopamine receptors and calcium channels has been characterized in radioligand binding and electrophysiological studies.
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| ln Vivo |
In vivo, tetrahydropalmatine possesses analgesic effects in animal models. It acts through inhibition of amygdaloid release of dopamine to inhibit epileptic attack in rats. The compound is used in traditional Chinese medicine for the treatment of pain, insomnia, and other conditions. Its sedative and analgesic effects have been documented in preclinical and clinical studies.
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| Enzyme Assay |
In vitro receptor binding assays for tetrahydropalmatine measure its affinity for dopamine D1 and D2 receptors. Membranes prepared from cells expressing the receptors are incubated with radiolabeled dopamine receptor ligands (e.g., [3H]-SCH23390 for D1, [3H]-spiperone for D2) and varying concentrations of the compound. The binding affinity (Ki) is calculated from competitive binding curves. Functional assays measure receptor activation or inhibition using cAMP accumulation or other downstream readouts.
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| Cell Assay |
In vitro cell-based assays for tetrahydropalmatine use neuronal cell lines or primary neurons. Cells are treated with serial dilutions of the compound, and effects on dopamine receptor signaling are measured by cAMP accumulation or calcium flux. L-type calcium channel activity is assessed using patch-clamp electrophysiology or calcium imaging with fluorescent indicators. Cell viability and toxicity are assessed in parallel.
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| Animal Protocol |
In vivo animal models for tetrahydropalmatine include rat models of pain (e.g., hot plate test, tail flick test) and epilepsy. The compound is administered orally or intraperitoneally, and its analgesic or anticonvulsant effects are evaluated. In the epilepsy model, tetrahydropalmatine inhibits epileptic attacks through inhibition of amygdaloid dopamine release. Dose-response studies establish the effective dose for pain relief or seizure inhibition.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of tetrahydropalmatine have been characterized in preclinical studies. The compound is absorbed following oral administration and distributes to various tissues. It is metabolized in the liver and excreted via urine. Its half-life, bioavailability, and tissue distribution are documented in the pharmacokinetic literature. The compound is stable when stored protected from light.
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| Toxicity/Toxicokinetics |
Toxicity data for tetrahydropalmatine are available from preclinical safety studies. The compound is generally well-tolerated at therapeutic doses. Common adverse effects may include sedation, dizziness, and gastrointestinal disturbances. High doses may cause respiratory depression. The compound is not recommended for use in pregnant women due to insufficient safety data.
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| Additional Infomation |
2,3,9,10-Tetramethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinoline is an alkaloid. Tetrahydropalmatine is currently being studied in the clinical trial NCT02118610 (L-Tetrahydropalmatine (L-THP) for the treatment of schizophrenia: a novel dopamine antagonist with anti-inflammatory and antiprobiotic activities). Rotundine has been reported in Stephania tetrandra, Stephania delavayi, and other organisms with relevant data.
Tetrahydropalmatine is an isoquinoline alkaloid used in traditional Chinese medicine for its analgesic and sedative properties. It is also known as rotundine or THP. The compound acts as a dopamine receptor antagonist and L-type calcium channel blocker. It is used for the treatment of pain, insomnia, and dysmenorrhea. Research continues into its potential applications in neurology and psychiatry. |
| Molecular Formula |
C21H25NO4
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|---|---|
| Molecular Weight |
355.43
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| Exact Mass |
355.178
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| Elemental Analysis |
C, 70.96; H, 7.09; N, 3.94; O, 18.01
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| CAS # |
10097-84-4
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| Related CAS # |
4880-82-4 (HCl); 10097-84-4
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| PubChem CID |
5417
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| Appearance |
Solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
482.9±45.0 °C at 760 mmHg
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| Flash Point |
138.7±25.9 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.609
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
475
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC=C2CC3N(CC2=C1OC)CCC1=CC(=C(C=C31)OC)OC
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| InChi Key |
AEQDJSLRWYMAQI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H25NO4/c1-23-18-6-5-13-9-17-15-11-20(25-3)19(24-2)10-14(15)7-8-22(17)12-16(13)21(18)26-4/h5-6,10-11,17H,7-9,12H2,1-4H3
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| Chemical Name |
2,3,9,10-tetramethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinoline
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| Synonyms |
Caseanine; Rotundine; Tetrahydropalmatine; (-)-Tetrahydropalmatine; (S)-Tetrahydropalmatine; L-Tetrahydropalmatine
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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 | 2.8135 mL | 14.0675 mL | 28.1349 mL | |
| 5 mM | 0.5627 mL | 2.8135 mL | 5.6270 mL | |
| 10 mM | 0.2813 mL | 1.4067 mL | 2.8135 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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