Cat. No.: HY-N0480

Reserpine

Name: Reserpine
Brand: MedChemExpress
SKU: HY-N0480
Price: 66.00 USD
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9 Cited Publications

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

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Pureté : 99.92%
CAS No.: 50-55-5
Formule: C₃₃H₄₀N₂O₉
Masse moléculaire:608.68

Stockage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Reserpine Chemical Structure

CAS No.: 50-55-5

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Induced Disease Models
- Essai clinique
Chemical Information
Publications (9)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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

IC₅₀ & Target

VMAT2^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	15.5 nM Compound: 5770	Substrate uptake and inhibition of the Vesicular Amine Transporter 2 (VMAT2, SLC18A2) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A2 cells Substrate uptake and inhibition of the Vesicular Amine Transporter 2 (VMAT2, SLC18A2) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A2 cells	10.5281/zenodo.7360403
HEK293	IC₅₀	15.5 nM Compound: 5770	Substrate uptake and inhibition of the Vesicular Amine Transporter 2 (VMAT2, SLC18A2) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A2 cells (PubChem AID: 1794817) Substrate uptake and inhibition of the Vesicular Amine Transporter 2 (VMAT2, SLC18A2) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A2 cells (PubChem AID: 1794817)	10.5281/zenodo.7360403
HEK293	IC₅₀	50 nM Compound: 5770	Substrate uptake and inhibition of the chromaffin granule amine transporter (VAT1, VMAT1, SLC18A1) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A1 cells Substrate uptake and inhibition of the chromaffin granule amine transporter (VAT1, VMAT1, SLC18A1) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A1 cells	10.5281/zenodo.7360413
HEK293	IC₅₀	50 nM Compound: 5770	Substrate uptake and inhibition of the chromaffin granule amine transporter (VAT1, VMAT1, SLC18A1) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A1 cells (PubChem AID: 1794818) Substrate uptake and inhibition of the chromaffin granule amine transporter (VAT1, VMAT1, SLC18A1) as assessed by uptake of a fluorescent substrate (FFN206) in HEK-293 JumpIN-SLC18A1 cells (PubChem AID: 1794818)	10.5281/zenodo.7360413
HEp-2	ED₅₀	>20 μg/mL Compound: Reserpin	Cytotoxicity against human Hep2 cells after 72 hrs Cytotoxicity against human Hep2 cells after 72 hrs	[PMID: 18500841]
HL-60	IC₅₀	67 μM Compound: 8	Cytotoxicity against human HL60 cells by MTT assay Cytotoxicity against human HL60 cells by MTT assay	[PMID: 15974606]
MCF7	IC₅₀	0.003 μg/mL Compound: Reserpine	Cytotoxicity against vinblastin-sensitive human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against vinblastin-sensitive human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 25536852]
MCF7	IC₅₀	0.037 μg/mL Compound: Reserpine	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 25536852]
MCF7	IC₅₀	0.31 μg/mL Compound: Reserpine	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay in presence of vinblastine Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay in presence of vinblastine	[PMID: 25536852]
MRC5	GI₅₀	14.7 μM Compound: Reserpine	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29597171]
NIH-3T3-G185	IC₅₀	0.5 μM Compound: Reserpine	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	2.1 μM Compound: Reserpine	TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	2.1 μM Compound: Reserpine	TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	2.6 μM Compound: Reserpine	TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	3.9 μM Compound: Reserpine	TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	5.3 μM Compound: Reserpine	TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	6.1 μM Compound: Reserpine	TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
Vero C1008	CC₅₀	25 μM Compound: 70	Cytotoxicity against African green monkey Vero E6 cells incubated for 2 days by the MTS assay Cytotoxicity against African green monkey Vero E6 cells incubated for 2 days by the MTS assay	[PMID: 32845145]

In Vitro

Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2). Reserpine displays a significant effect 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 in JB6 P+ and HepG2-C8 cells, respectively. Reserpine 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 (2.5 to 10 μM) also increases the protein expression of Nrf2, HO-1, and NQO1. Reserpine 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 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].

1. 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.

2. 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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 50-55-5
Appearance Solid
Masse moléculaire 608.68
Formule C₃₃H₄₀N₂O₉
Color White to light 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
Structure Classification
- Alkaloids
- Piperidine Alkaloids
- Alkaloids
- Indole Alkaloids
Initial Source
- Plants
- Other Families Extract
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (9)

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Phytomedicine

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

2024 Dec:135:156002. PMID: 39326134

Reserpine 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 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 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
Microorganisms

2026 Aug 14;14(8):1792. PMID: 42655135
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 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 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.

Solvant et solubilité

In Vitro:

DMSO : 31.82 mg/mL (52.28 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.6429 mL

8.2145 mL

16.4290 mL

5 mM

0.3286 mL

1.6429 mL

3.2858 mL

10 mM

0.1643 mL

0.8214 mL

1.6429 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

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Volume Volume

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Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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Volume _(final) Volume _(final)

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 (4.11 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 (4.11 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.

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

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
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Instruction de manipulation (2659 KB)

Références

[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	1.6429 mL	8.2145 mL	16.4290 mL	41.0725 mL
	5 mM	0.3286 mL	1.6429 mL	3.2858 mL	8.2145 mL
	10 mM	0.1643 mL	0.8214 mL	1.6429 mL	4.1072 mL
	15 mM	0.1095 mL	0.5476 mL	1.0953 mL	2.7382 mL
	20 mM	0.0821 mL	0.4107 mL	0.8214 mL	2.0536 mL
	25 mM	0.0657 mL	0.3286 mL	0.6572 mL	1.6429 mL
	30 mM	0.0548 mL	0.2738 mL	0.5476 mL	1.3691 mL
	40 mM	0.0411 mL	0.2054 mL	0.4107 mL	1.0268 mL
	50 mM	0.0329 mL	0.1643 mL	0.3286 mL	0.8214 mL

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Keywords

Reserpine

9 Cited Publications

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Reserpine

Publications Citing Use of MedChemExpress (MCE) Reserpine