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  5. Gastric Ulcer Models
  6. Reserpine hydrochloride

Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

For research use only. We do not sell to patients.

CAS No. : 16994-56-2

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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Reserpine hydrochloride:

Reserpine hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Reserpine hydrochloride purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2024 Dec:135:156002.

    Reserpine (Res) (0.375 mg/kg; i.g.) administration resulted in down-regulation of m6A in xenograft tumors derived from Huh7/Len cells.

    Reserpine hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Jul:176:116856.  [Abstract]

    Reserpine (0.25 mg/kg; s.c.; 3 d) injection caused fibromyalgia mice to exhibit mechanical hyperalgesia compared to the sham group, evidenced by a decrease in the paw withdraw threshold (PWT) after ciliary stimulation along with a decrease in thermal pain latency and higher sensitivity to cold pain after acetone stimulation.

    Reserpine hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Jul:176:116856.  [Abstract]

    Reserpine (0.25 mg/kg; s.c.; 3 d) significantly increased the immobility time in the tail suspension test (TST) and forced swimming test (FST) of fibromyalgia mice.

    Reserpine hydrochloride purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2024 Sep;131(5):918-930.  [Abstract]

    Reserpine (10 μM; 2  h) functionally inhibited ABCB1 (PgP) multi-drug transporters in 4 studied cell lines and patient-derived primary cells.

    Reserpine hydrochloride purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2024 Sep;131(5):918-930.  [Abstract]

    Reserpine (10 μM; 2  h) potently inhibited ABCB1 and the efflux of MTG in MDA-MB-231 cells.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).

    IC50 & Target

    VMAT2[1]
    In Vitro

    Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2). Reserpine hydrochloride displays a significant on the density of dopamine D1 receptors (F2,12=8.81, p<0.01) in the rat striatum. The affinity (Kd) for the dopamine D1 and D2 receptors during withdrawal from acute and chronic administration of reserpine is not change[1]. IC50 values of 43.9 and 54.9 μM are obtained after 1 day of treatment with Reserpine hydrochloride in JB6 P+ and HepG2-C8 cells, respectively. Reserpine hydrochloride induces luciferase activity in a dose-dependent manner at concentrations ranging from 5 to 50 μM, and no significant induction is observed at concentrations lower than 5 μM. Results demonstrate that Reserpine hydrochloride (2.5 to 10 μM) also increases the protein expression of Nrf2, HO-1, and NQO1. Reserpine hydrochloride at concentrations of 2.5 to 10 μM decreases the mRNA expression of DNMT1, DNMT3a, and DNMT3b in a concentration-dependent manner in JB6 P+ cells after 7 days of treatment. Reserpine hydrochloride at 10 μM generates a significant difference for DNMT3a expression (p<0.05)[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Reserpine hydrochloride Related Antibodies
    In Vivo

    Note:
    Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

    Reserpine can be used in animal modeling to create gastrointestinal ulcer and depression models. Withdrawal from chronic (14 days) but not acute reserpine (48 hours) significantly decreases immobility time (F2,18=3.68, p<0.05) and increases climbing time (F2,18=4.48, p<0.02) in rats, without altering swimming time in the forced swim test (FST) (F2,18=1.78; NS) compared to control animals. A dose of 5 mg/kg body weight of Reserpine significantly increases the urinary excretion of vanillylmandelic acid (VMA). Animals treated with Reserpine excrete more 5-hydroxyindoleacetic acid (5-HIAA) than controls. Reserpine treatment results in dose-dependent hypotension. Compared to controls, doses of 0.5, 1, 5, 10, and 15 μg/kg of Reserpine significantly (p<0.01) reduce blood pressure[1][3].

    Induction of Gastric Ulcer[4][5][6]
    Background
    Peripheral cholinergic and adrenergic mechanisms are involved in the ulceration induced by reserpine. The ulcerogenic activity of reserpine was significantly reduced by α-adrenoceptor antagonists (phenoxybenzamine (HY-B0431) and phentolamine (HY-12717)) but not by the β-adrenoceptor blocker, propranolol (HY-B0573B)[6].
    Specific Modeling Methods
    Rat: Wistar Rats • male • 200-290 g[4]
    Administration: 5 mg/kg • ip • 18 h before sacrifice
    Mice: ICR mice • male • 7 weeks old[5]
    Administration: 10 mg/kg • ip • once daily for 3 days
    Note
    (1)Rats were fasted with water ad libitum for 48 h prior to experimentation. Rats were housed and experiments were conducted in a temperature-controlled room (23 ± 1°C).
    (2)The level of cancer induction was identified by specific biochemical markers such as serum gastrin level, TBARS, and glutathione followed by histopathological analysis at two-time periods for 8 and 16 week.
    Modeling Indicators
    Individual phenotypic changes: induced marked gastric glandular ulceration and elicited the release of free /~-glucuronidase from lysosomes in the gastric mucosa.
    Molecular changes: In the reserpine-induced gastric ulcer control mice, the gastric secretion volume was increased, the pH value (1.04) was decreased, the serum cytokine levels of IL-6, IL-12, TNF-α and IFN-γ was increased.

    Induction of Depression[7][8]
    Background
    Reserpine is an irreversible inhibitor of vesicular monoamine transporter 2, which regulates the accumulation of monoamines into the synaptic vesicles and their reuptake from the synapses. Therefore, Reserpine inhibits monoamine pre-synaptic reuptake and storage, leading to monoamine depletion and depressive disorders[7].
    Specific Modeling Methods
    Rat: Wistar Rats • male • 120-150 g[7]
    Administration: 0.5 mg/kg • ip • once per day for 14 days
    Mice: C57BL/6 mice • male • 7 weeks old[8]
    Administration: 0.5 mg/kg • ip • once per day for 10 days
    Note
    (1) Reserpine was diluted in glacial acetic acid to a final concentration of 0.5% acetic acid in distilled water.
    Modeling Indicators
    Individual phenotypic changes: showed a significant decrease in spontaneous locomotor activity in the activity cage, decrease in latency to immobility, and increase in the immobility duration in forced swimming test (FST), indicating motor impairment and worsened depressive phenotype.
    Molecular changes: Reserpine administration significantly increased cortical contents of MDA (malondialdehyde), reduced GSH (glutathione), increased TNF-ɑ and reduced BDNF (brain derived neurotropic factor). Showed a significant decrease in cortical nor-epinephrine (NE), serotonin (5-HT), and dopamine (DA)

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    645.14

    Formula

    C33H41ClN2O9
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    O=C([C@H]([C@@H](OC)[C@H](OC(C1=CC(OC)=C(OC)C(OC)=C1)=O)C[C@]2([H])CN3CC4)[C@@]2([H])C[C@]3([H])C5=C4C(C=CC(OC)=C6)=C6N5)OC.Cl
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (77.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5501 mL 7.7503 mL 15.5005 mL
    5 mM 0.3100 mL 1.5501 mL 3.1001 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (3.88 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.88 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    % 
    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.89%

    SDS (394 KB)

    COA (251 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [2]

    After incubation for 24 h, JB6 P+ cells (1×105 cells/10-cm dish) are treated with various concentrations of Reserpine hydrochloride. Whole cell lysates are prepared from the treated cells using radioimmunoprecipitation assay buffer supplemented with a protease inhibitor cocktail, and a BCA kit is used to determine protein concentrations[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [2]

    JB6 P+ cells are seeded in 96-well plates containing Minimum essential media (MEM) at a density of 1×104 cells/mL (100 μL/well) for 1, 3, and 5 days, and HepG2-C8 cells are seeded in plates containing DMEM. After incubation for 24 h, the cells are treated with either DMSO or various concentrations of Reserpine hydrochloride. For JB6 P+ cells, the medium is changed every 2 days for the 3-day and 5-day treatments. Cell viability is assessed using a MTS assay kit according to the manufacturer’s instructions. The absorbance of the formazan product is read at 490 nm, and the cell viability is calculated and compared with the DMSO control group[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Albino rats of either sex weighing between 100 to 150 g are used in the study. They are acclimatized to the laboratory conditions for at least 10 days prior to the experiment and are provided with standard diet and water ad libitum with 12 h light and dark cycle. Animals are divided into different groups of six each and are housed individually in metabolic cages. Group 1: Control animals treated with DMSO intraperitoneally at a dose of 0.1 mL/100 g body weight. Group 2: Animals administered intraperitoneally with Reserpine hydrochloride at a dose of 5 mg/kg body weight. The 24 h urine samples from the point of drug administration are collected for each animal[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5501 mL 7.7503 mL 15.5005 mL 38.7513 mL
    5 mM 0.3100 mL 1.5501 mL 3.1001 mL 7.7503 mL
    10 mM 0.1550 mL 0.7750 mL 1.5501 mL 3.8751 mL
    15 mM 0.1033 mL 0.5167 mL 1.0334 mL 2.5834 mL
    20 mM 0.0775 mL 0.3875 mL 0.7750 mL 1.9376 mL
    25 mM 0.0620 mL 0.3100 mL 0.6200 mL 1.5501 mL
    30 mM 0.0517 mL 0.2583 mL 0.5167 mL 1.2917 mL
    40 mM 0.0388 mL 0.1938 mL 0.3875 mL 0.9688 mL
    50 mM 0.0310 mL 0.1550 mL 0.3100 mL 0.7750 mL
    60 mM 0.0258 mL 0.1292 mL 0.2583 mL 0.6459 mL
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    Reserpine hydrochloride Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Reserpine16994-56-2Monoamine TransporterInhibitorinhibitorinhibit

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