[CAS NO. 50-55-5] Reserpine
PRODUCTS SPECIFICATIONS [50-55-5]
DESCRIPTION [50-55-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 608.68 |
| Molecular Formula | C33H40N2O9 |
| 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 |
2 Publications Citing Use of MCE
Summary
Reserpine is an inhibitor of the vesicular monoamine transporter 2 ( VMAT2 ).
IC50 & Target
VMAT2 [1]
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] . IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Withdrawal (48 h) from chronic (14-day) but not acute Reserpine administration in a dose of 0.2 mg/kg i.p. produces a significant reduction of the immobility time (F 2,18 =3.68, p<0.05), but increases the climbing time (F 2,18 =4.48, p<0.02), and does not change the swimming time (F 2,18 =1.78; NS) in the forced swim test (FST) in rats [1] . Reserpine at a dose of 5 mg/kg body weight produces significant increase in the urinary excretion profile of vanillylmandelic acid (VMA) compare to control animals. The amount of 5-hydroxyindoleacetic acid (5-HIAA) excreted in animals treated with Reserpine is found to be more than in the control. Dose dependent hypotension is observed with Reserpine. Reserpine at doses of 0.5, 1, 5, 10 and 15 μg/kg produce significant (p<0.01) reduction in blood pressure compare to control [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00000514 | National Heart, Lung, and Blood Institute (NHLBI)|National Institute on Aging (NIA) |
Cardiovascular Diseases|Cerebrovascular Disorders|Heart Diseases|Hypertension
|
June 1984 | Phase 3 |
| NCT03223272 | University of Alabama at Birmingham |
Refractory Hypertension
|
July 23, 2015 | Phase 2 |
| NCT00000499 | National Heart, Lung, and Blood Institute (NHLBI)|National Institute on Aging (NIA) |
Cardiovascular Diseases|Heart Diseases|Hypertension|Vascular Diseases
|
September 1980 | Phase 2 |
| NCT00267657 | National Institute on Drug Abuse (NIDA) |
Amphetamine-Related Disorders
|
January 2004 | Phase 1 |
| NCT02684786 | Mayo Clinic |
Pulmonary Artery Hypertension
|
July 2016 | Phase 1 |
| NCT00033033 | National Institute on Drug Abuse (NIDA)|Cincinnati VA Medical Center |
Cocaine-Related Disorders|Substance-Related Disorders
|
July 2001 | Phase 2 |
Appearance
Solid
Source
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 25 mg/mL ( 41.07 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 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 |
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.11 mM); Clear solution
References
- [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.
- [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.
- [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.
Synonyms