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    CAS No. 2934-97-6 Price $30 / 20mg
    Catalog No.CFN99553Purity>=98%
    Molecular Weight355.42Type of CompoundAlkaloids
    FormulaC21H25NO4Physical DescriptionPowder
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  • Biological Activity
    Description: Tetrahydropalmatine, a plant alkaloid used as an ingredient in dietary supplement products, is a potent and selective D1 receptor antagonist. Tetrahydropalmatine shows a promyogenic effect by upregulation of p38MAPK, Akt resulting in enhanced MyoD activation, it can effectively protect endothelial cells against γ-irradiation injury. Tetrahydropalmatine has a potential as a therapeutic candidate to prevent fibrosis and improve muscle regeneration and repair and applied to the prevention of endothelial cell dysfunctions associated with ionizing irradiation-induced lung injury.
    Targets: GABA receptor | p38MAPK | Akt | 5-HT Receptor | Bcl-2/Bax | Caspase
    In vitro:
    Life Sci. 2010 Jul 3;87(1-2):55-63.
    Protective effects of tetrahydropalmatine against gamma-radiation induced damage to human endothelial cells.[Pubmed: 20562023 ]
    Irradiation-induced damage to pulmonary endothelial cells is thought to be an important mediator of the pathogenesis of radiation pneumonopathy. Tetrahydropalmatine (THP) has been shown to have a protective effect against oxidative stress. This study was designed to investigate the potential radioprotective effect of THP against irradiation-induced endothelial cellular damage and to elucidate the underlying mechanisms.
    Human EA.hy926 cells were treated with THP and irradiation. Cell viability was measured using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. For the detection of apoptosis, morphological observation, flow cytometry and a caspase-3 activity assay were employed. The expression of cytochrome-c and Bax/Bcl-2 protein were detected by western blot analysis. Generation of reactive oxygen species (ROS) was measured by flow cytometry. Malondialdehyde (MDA), lactate dehydrogenase (LDH), glutathione (GSH) and superoxide dismutase (SOD) were measured to assess cellular oxidative stress induced injury. Preincubation of EA.hy926 cells with THP before gamma-radiation resulted in significant inhibition of apoptosis and enhancement of cell viability, as revealed by morphological observation, flow cytometry and MTT assay. THP significantly reduced intracellular ROS formation, levels of intracellular MDA and LDH, and enhanced the production of intracellular antioxidants (GSH and SOD) in EA.hy926 cells. Meanwhile, THP also inhibited the decrease of intracellular mitochondrial membrane potential (psim), caspase-3 activation, cytochrome-c release and reduced Bax/Bcl-2 ratio in THP pretreated, irradiated cells.
    Our findings demonstrated THP could effectively protect endothelial cells against gamma-irradiation injury, which could potentially be applied to the prevention of endothelial cell dysfunctions associated with ionizing irradiation-induced lung injury.
    In vivo:
    Phytomedicine. 2014 Sep 25;21(11):1287-91.
    L-tetrahydropalmatine inhibits methamphetamine-induced locomotor activity via regulation of 5-HT neuronal activity and dopamine D3 receptor expression.[Pubmed: 25172791]
    Methamphetamine (METH) is a psychomotor stimulant that produces hyperlocomotion in rodents. l-Tetrahydropalmatine (l-THP) is an active ingredient found in Corydalis ternata which has been used as a traditional herbal preparation in Asian countries for centuries, however, the effect of l-THP on METH-induced phenotypes largely unknown.
    In this study, to evaluate the effect of l-THP on METH-induced psychotropic effects, rats were pretreated with l-THP (10 and 15 mg/kg) before acute METH injection, following which the total distance the rats moved in an hour was measured. To clarify a possible mechanism underlying the effect of l-THP on METH-induced behavioral changes, dopamine receptor mRNA expression levels in the striatum of the rats was measured following the locomotor activity study. In addition, the effect of l-THP (10 and 15 mg/kg) on serotonergic (5-HTergic) neuronal pathway activation was studied by measurement of 5-HT (80 μg/10μl/mouse)-induced head twitch response (HTR) in mice. l-THP administration significantly inhibited both hyperlocomotion in rats and HTR in mice. l-THP inhibited climbing behavior-induced by dopaminergic (DAergic) neuronal activation in mice. Furthermore, l-THP attenuated the decrease in dopamine D3 receptor mRNA expression levels in the striatum of the rats induced by METH.
    These results suggest that l-THP can ameliorate behavioral phenotype induced by METH through regulation of 5-HT neuronal activity and dopamine D3 receptor expression.
    Neuropharmacology. 2007 Nov;53(6):771-82.
    Levo-tetrahydropalmatine inhibits cocaine's rewarding effects: experiments with self-administration and brain-stimulation reward in rats[Pubmed: 17888459 ]
    It was recently reported that levo-Tetrahydropalmatine (l-THP), a dopamine (DA) D1 and D2 receptor antagonist purified from the Chinese herb Stephanie, appears to be effective in attenuating cocaine self-administration, cocaine-triggered reinstatement and cocaine-induced conditioned place preference in preclinical animal models.
    The present study was designed to contrast l-THP's effects on cocaine self-administration under fixed-ratio (FR) and progressive-ratio (PR) reinforcement, and to study l-THP's effects on cocaine-enhanced brain stimulation reward (BSR). Systemic administration of l-THP produced dose-dependent, biphasic effects, i.e., low-to-moderate doses (1, 3, 10 mg/kg) increased, while a high dose (20 mg/kg) inhibited cocaine self-administration behavior under FR2 reinforcement. The increased cocaine self-administration is likely a compensatory response to a reduction in cocaine's rewarding effects, because the same low doses of l-THP dose-dependently attenuated cocaine self-administration under PR reinforcement and also attenuated cocaine-enhanced BSR. These attenuations of PR cocaine self-administration and cocaine-enhanced BSR are unlikely due to l-THP-induced sedation or locomotor inhibition, because only 10 mg/kg, but not 1-3 mg/kg, of l-THP inhibited locomotion, sucrose self-administration and asymptotic operant performance in the BSR paradigm. In vivo microdialysis demonstrated that l-THP slightly elevates extracellular nucleus accumbens DA by itself, but dose-dependently potentiates cocaine-augmented DA, suggesting that a postsynaptic, rather than presynaptic, DA receptor antagonism underlies l-THP's actions on cocaine reward.
    Together, the present data, combined with previous findings, support the potential use of l-THP for treatment of cocaine addiction.
    Tetrahydropalmatine Description
    Source: The tubers of Corydalis yanhusuo W. T. Wang ex Z. Y. Su et C. Y. Wu
    Solvent: Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
    Storage: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com

    After receiving: The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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    Calculate Dilution Ratios(Only for Reference)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.8136 mL 14.0679 mL 28.1357 mL 56.2715 mL 70.3393 mL
    5 mM 0.5627 mL 2.8136 mL 5.6271 mL 11.2543 mL 14.0679 mL
    10 mM 0.2814 mL 1.4068 mL 2.8136 mL 5.6271 mL 7.0339 mL
    50 mM 0.0563 mL 0.2814 mL 0.5627 mL 1.1254 mL 1.4068 mL
    100 mM 0.0281 mL 0.1407 mL 0.2814 mL 0.5627 mL 0.7034 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    Cell Research:
    Biochem Biophys Res Commun. 2014 Dec 12;455(3-4):147-52.
    Tetrahydropalmatine promotes myoblast differentiation through activation of p38MAPK and MyoD.[Pubmed: 25450677]
    Myoblast differentiation is fundamental to the development and regeneration of skeletal muscle after injury or disease. MyoD family transcription factors play a key role to promote myoblast differentiation.
    In a screen for MyoD activators, we identified Tetrahydropalmatine (THP), a natural compound isolated from Corydalis turtschaninovii. The treatment of C2C12 myoblasts with THP enhanced the level of MyoD, Myogenin and myosin heavy chain (MHC) proteins and the formation of larger multinucleated myotubes, compared to the control treatment. The THP treatment dramatically enhanced the activities of p38MAPK and Akt, the key promyogenic kinases which activate MyoD. The enhanced myoblast differentiation by THP treatment can be blocked by inhibition of p38MAPK or Akt by SB203580 or LY294002, respectively. In addition, THP treatment restored myotube formation of Cdo-depleted C2C12 cells through activation of p38MAPK. Moreover, THP enhanced the efficiency of trans-differentiation of 10T1/2 fibroblasts into myoblasts mediated by MyoD. These results indicate that THP has a promyogenic effect by upregulation of p38MAPK and Akt resulting in enhanced MyoD activation.
    Our findings suggest that THP has a potential as a therapeutic candidate to prevent fibrosis and improve muscle regeneration and repair.
    Animal Research:
    Prog Neuropsychopharmacol Biol Psychiatry. 2003 Aug;27(5):775-9.
    Anxiolytic-like action of orally administered dl-tetrahydropalmatine in elevated plus-maze.[Pubmed: 12921909]
    dl-Tetrahydropalmatine (dl-THP), a naturally occurring alkaloid, has been intensively studied for its sedative and hypnotic effects. Putative explanation for its mechanism and target of action involves the dopaminergic neurotransmission system. In view of the close interactions between the dopaminergic and the GABAergic neurons in the amygdala, pharmacological effects of dl-THP were tested for activity at the GABAA receptor benzodiazepine site (BDS).
    Effects of dl-THP were examined in mice employing the elevated plus-maze, the holeboard and the horizontal-wire tests. In the elevated plus-maze, mice treated with low doses of dl-THP (0.5-10 mg/kg) exhibited significant increase in the percentage of entries and time spent in open arms without altering the number of closed-arm entries when compared to the control group, indicative of its selective anxiolytic effect. In the holeboard and horizontal wire tests, where exploratory behavior and potential muscle relaxant effect were assessed, respectively, only mice treated with as much as 50 mg/kg dl-THP manifested sedation and myorelaxation, as observed in the significant decrease in the number of head dips and the decrease in the percentage of mice grasping wire in comparison to control. Notably, coadministration of the BDS antagonist flumazenil abolished the dl-THP-induced anxiolysis as seen in the reversal of the increase of both the number of entries and time spent in open arms back to basal levels in the elevated plus-maze test.
    The results suggest that dl-THP at defined low dosages acts as anxiolytics in mice, and the BDS mediates, at least in part, such anxiolytic effect of dl-THP.
    Clin Exp Pharmacol Physiol. 1996 Aug;23(8):738-42.
    Antihypertensive effects of DL-tetrahydropalmatine: an active principle isolated from Corydalis.[Pubmed: 8886500]
    1. The effects of DL-Tetrahydropalmatine (DL-THP) on cardio-vascular function and hypothalamic release of monoamines were assessed in rats under urethane anaesthesia.
    2. Intravenous administration of DL-THP (1-10 mg/kg) produced hypotension, bradycardia, a decrease in hypothalamic serotonin and noradrenaline release and an increase in hypothalamic dopamine release in rats. 3. Intrahypothalamic administration of DOI (a serotonergic 5-HT2 receptor antagonist) or apomorphine (a dopamine D2-receptor agonist) produced the opposite effects and reversed DL-THP-induced hypotension and bradycardia.
    4. The data suggest that DL-THP acts through the 5-HT2 and/or D2-receptor antagonism in the hypothalamus to induce hypotension and bradycardia in rats.