Art. -Nr.: HY-N0480A

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Reserpine hydrochloride

8 Cited Publications

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

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Reinheit: 99.87%
CAS. Nr.: 16994-56-2
Formel: C₃₃H₄₁ClN₂O₉
Molecular Weight:645.14

Speicherung:

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)

Reserpine hydrochloride Chemical Structure

CAS. Nr.: 16994-56-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Induced Disease Models
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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 (F_2,12=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.

Induced Disease Models

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 (F_2,18=3.68, p<0.05) and increases climbing time (F_2,18=4.48, p<0.02) in rats, without altering swimming time in the forced swim test (FST) (F_2,18=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.

Chemical Information

CAS. Nr. 16994-56-2
Appearance Solid
Molecular Weight 645.14
Formel C₃₃H₄₁ClN₂O₉
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
- Alkaloids
- Indole Alkaloids
Initial Source
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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)

Publications (8)

All Flow CytometryIn Vivo Efficacy StudyBio/Physico-chemical Assay

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Journal Impact Factor

Phytomedicine

Reserpine, a novel N6-methyladenosine regulator, reverses Lenvatinib resistance in hepatocellular carcinoma. [Abstract]

2024 Dec:135:156002. PMID: 39326134

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

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

HIV-protease inhibitors potentiate the activity of carfilzomib in triple-negative breast cancer. [Abstract]

2024 Sep;131(5):918-930. PMID: 38969867

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.
Crit Rev Anal Chem

A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]

2022;52(7):1557-1571. PMID: 33691566
Sci Rep

Lactate reprograms PGE2 metabolism via GPR81 inhibits COX2 to relieved psoriasis. [Abstract]

2026 May 6;16(1):20905. PMID: 42092124
Ren Fail

Reserpine alleviates cisplatin-induced acute kidney injury via anti-ferroptosis and cGAS/STING pathway. [Abstract]

2024 Dec;46(2):2406395. PMID: 39377110
ACS Chem Biol

2026 Apr 3;21(4):764-778.
F1000Res

2025.
Biomed Pharmacother

Astaxanthin alleviates fibromyalgia pain and depression via NLRP3 inflammasome inhibition. [Abstract]

2024 Jul:176:116856. PMID: 38852510

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.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5501 mL

7.7503 mL

15.5005 mL

5 mM

0.3100 mL

1.5501 mL

3.1001 mL

10 mM

0.1550 mL

0.7750 mL

1.5501 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.22 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (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].

MedChemExpress (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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (292 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Antkiewicz-Michaluk L, et al. Withdrawal from repeated administration of a low dose of reserpine induced opposing adaptive changes in the noradrenaline and serotonin system function: a behavioral and neurochemical ex vivo and in vivo studies in the rat. Prog Neuropsychopharmacol Biol Psychiatry. 2015 Mar 3;57:146-54. [Content Brief]

[2]. Hong B, et al. Reserpine Inhibit the JB6 P+ Cell Transformation Through Epigenetic Reactivation of Nrf2-Mediated Anti-oxidative Stress Pathway. AAPS J. 2016 May;18(3):659-69. [Content Brief]

[3]. Sreemantula S, et al. Reserpine methonitrate, a novel quaternary analogue of reserpine augments urinary excretion of VMA and 5-HIAA without affecting HVA in rats. BMC Pharmacol. 2004 Nov 16;4:30. [Content Brief]

[4]. Pfeiffer CJ, et al. Reserpine-induced gastric ulcers: protection by lysosomal stabilization due to zinc. Eur J Pharmacol. 1980 Feb;61(4):347-53. [Content Brief]

[5]. Li GJ, et al. Preventive Effect of Polysaccharide of Larimichthys crocea Swim Bladder on Reserpine Induced Gastric Ulcer in ICR Mice. Korean J Physiol Pharmacol. 2014 Apr;18(2):183-90. [Content Brief]

[6]. Gupta MB, et al. Mechanism of ulcerogenic activity of reserpine in albino rats. Eur J Pharmacol. 1974 Jul;27(2):269-71. [Content Brief]

[7]. Park BK, et al. Antidepressant-Like Effects of Gyejibokryeong-hwan in a Mouse Model of Reserpine-Induced Depression. Biomed Res Int. 2018 Jun 26;2018:5845491. [Content Brief]

[8]. El-Marasy SA, et al. Anti-depressant effect of cerebrolysin in reserpine-induced depression in rats: Behavioral, biochemical, molecular and immunohistochemical evidence. Chem Biol Interact. 2021 Jan 25;334:109329. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Reserpine hydrochloride

8 Cited Publications

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Reserpine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Reserpine hydrochloride

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Reserpine hydrochloride Related Classifications

HY-N0480A Related Classifications