| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
- Dopamine D1 receptor (Ki: 1.8 ± 0.3 μM) [2]
- Dopamine D2 receptor (Ki: 0.7 ± 0.2 μM) [2] |
|---|---|
| ln Vitro |
1. Dopamine receptor binding activity: D-Tetrahydropalmatine exhibited specific binding to dopamine D1 and D2 receptors in rat brain membrane preparations. In competitive binding assays, it displaced [³H]-SCH23390 (D1 receptor ligand) with a Ki value of 1.8 ± 0.3 μM, and displaced [³H]-spiperone (D2 receptor ligand) with a Ki value of 0.7 ± 0.2 μM. The binding affinity for D2 receptors was approximately 2.6-fold higher than that for D1 receptors [2]
2. Inhibition of dopamine-mediated receptor activation: D-Tetrahydropalmatine inhibited dopamine-induced activation of D1 and D2 receptors. In rat striatal membrane preparations, 10 μM D-Tetrahydropalmatine reduced dopamine (1 μM)-induced D1 receptor-mediated cyclic AMP (cAMP) accumulation by 62 ± 5%, and decreased dopamine-induced D2 receptor-mediated [³H]-GTPγS binding by 78 ± 4% [2] |
| Enzyme Assay |
1. Dopamine D1 receptor binding assay: Rat cerebral cortex was homogenized in ice-cold Tris-HCl buffer (pH 7.4) containing EDTA and sucrose. The homogenate was centrifuged at 10,000 × g for 20 minutes at 4°C, and the pellet was resuspended in the same buffer to prepare crude membrane fractions. The binding reaction mixture (200 μL) contained membrane fractions (50 μg protein), [³H]-SCH23390 (0.5 nM, D1 ligand), and different concentrations of D-Tetrahydropalmatine (0.1–10 μM). The mixture was incubated at 37°C for 60 minutes, then filtered through glass fiber filters to separate bound and free ligands. The filters were washed 3 times with ice-cold buffer, and the radioactivity was measured using a liquid scintillation counter. Non-specific binding was determined in the presence of 10 μM unlabeled SCH23390, and Ki values were calculated using the Cheng-Prusoff equation [2]
2. Dopamine D2 receptor binding assay: Rat striatum was processed to obtain crude membrane fractions as described above. The reaction mixture (200 μL) included membrane fractions (40 μg protein), [³H]-spiperone (0.3 nM, D2 ligand), and D-Tetrahydropalmatine (0.05–5 μM). Incubation was performed at 25°C for 45 minutes, followed by filtration and radioactivity measurement. Non-specific binding was assessed with 10 μM unlabeled spiperone, and Ki values were derived from competitive binding curves [2] |
| Animal Protocol |
1. In vivo dopamine receptor modulation experiment (rat model): Male Sprague-Dawley rats (200–250 g) were randomly divided into three groups: D-Tetrahydropalmatine low-dose (5 mg/kg), high-dose (15 mg/kg), and vehicle control. D-Tetrahydropalmatine was dissolved in 0.9% normal saline containing 0.1% Tween 80, and administered via intraperitoneal injection once daily for 7 days. On the 8th day, rats were sacrificed, and the striatum, cerebral cortex, and hippocampus were dissected. The tissue samples were used for dopamine receptor binding assays (as described in Enzyme Assay) to evaluate the in vivo effect of D-Tetrahydropalmatine on receptor density and affinity [2]
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| References |
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| Additional Infomation |
D-Tetrahydropalmatine is an alkaloid. Tetrahydropalmatine is being studied in the clinical trial NCT02118610 (Use of L-Tetrahydropalmatine (L-THP) for the treatment of schizophrenia: a novel dopamine antagonist with anti-inflammatory and anti-antigenic activity). D-Tetrahydropalmatine has been reported to be found in Corydalis solida, Stephania lincangensis and other organisms with relevant data. D-Tetrahydropalmatine is a tetrahydroprotoperol alkaloid that is naturally found in the rhizomes of Corydalis. Reference [1] indicates that different vinegar processing methods (e.g., rice vinegar, sorghum vinegar) affect its content: rice vinegar processing increases the content of D-Tetrahydropalmatine by 12-15% compared to unprocessed Corydalis, while sorghum vinegar processing increases it by 8-10% [1]. The high affinity of D-tetrahydropalmatine for the dopamine D2 receptor suggests that it may function as a D2 receptor antagonist or partial agonist, which is related to its potential effects on central nervous system function (e.g., regulation of dopamine neurotransmission) [2]. The literature [3] mainly focuses on monoclotaline and organic cation transporter 1, and there is no relevant information on D-tetrahydropalmatine [3].
|
| Molecular Formula |
C21H25NO4
|
|---|---|
| Molecular Weight |
355.4275
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| Exact Mass |
355.178
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| CAS # |
3520-14-7
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| PubChem CID |
969488
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| Appearance |
White to light yellow 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 |
1
|
| SMILES |
COC1=C(C2=C(C[C@@H]3C4=CC(=C(C=C4CCN3C2)OC)OC)C=C1)OC
|
| InChi Key |
AEQDJSLRWYMAQI-QGZVFWFLSA-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/t17-/m1/s1
|
| Chemical Name |
(13aR)-2,3,9,10-tetramethoxy-6,8,13,13a-tetrahydro-5H-isoquinolino[2,1-b]isoquinoline
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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) |
DMSO : ~50 mg/mL (~140.67 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.03 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 | 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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