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Reserpine VMAT inhibitor

Cat.No.S1601

Reserpine is an inhibitor of multidrug efflux pumps, used as an antipsychotic and antihypertensive drug. This compound is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).It can be used to induce animal models of Gastric and Intestinal Ulcers.
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Quality Control

Batch: Purity: 99.77%
99.77

Solubility

In vitro
Batch:

DMSO : 13 mg/mL (21.35 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 608.68 Formula

C33H40N2O9

Storage (From the date of receipt)
CAS No. 50-55-5 Download SDF Storage of Stock Solutions

Synonyms N/A SMILES COC1C(CC2CN3CCC4=C(C3CC2C1C(=O)OC)NC5=C4C=CC(=C5)OC)OC(=O)C6=CC(=C(C(=C6)OC)OC)OC

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Mechanism of Action

In vitro
Reserpine inhibits efflux pumps and reduces sparfloxacin, moxifloxacin and ciprofloxacin IC50s and MICs by up to four-fold in 11, 21 and 48 of the 102 unrelated clinical isolates tested.
In vivo
Reserpine (5 mg/kg s.c.) reduces extracellular DA levels to 4% of basal values in intact rats. This compound diminishes L-DOPA (50 mg/kg i.p.)-induced increases in extracellular dopamine levels to 16% of those obtained in denervated animals not pretreated with reserpine in 6-hydroxydopamine-lesioned rats. It causes a marked depletion of vasopressin/oxytocin-neu-rophysin-like immunoreactivity (LI) and CRH-L1 in the median eminence of the rat. This chemical significantly restores performance on the delayed response task in monkeys. It has little effect on performance of a visual discrimination task, a reference memory task which does not depend on the prefrontal cortex. Its injection (one dose of 1 mg/kg s.c.) every other day for 3 days causes a significant increase in vacuous chewing, tongue protrusion and duration of facial twitching in rats, compared to the control. This agent results in a decreased glutamate uptake in the subcortical parts of rats. It (5 mg/kg) significantly increases vacuous jaw movements, and also reduces rearing behavior in all age groups of rats.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/8102313/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15649445/
  • [6] https://pubmed.ncbi.nlm.nih.gov/8265695/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-03-05)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06199778 TERMINATED
Traumatic Brain Injury
Zeng Changhao
2022-06-01
NCT03223272 COMPLETED
Refractory Hypertension
University of Alabama at Birmingham
2015-07-23 PHASE2
NCT02684786 WITHDRAWN
Pulmonary Artery Hypertension
Mayo Clinic
2016-07 PHASE1
NCT00000499 COMPLETED
Cardiovascular Diseases; Heart Diseases; Hypertension; Vascular Diseases
National Heart, Lung, and Blood Institute (NHLBI)
1980-09 PHASE2
NCT00000514 COMPLETED
Cardiovascular Diseases; Cerebrovascular Disorders; Heart Diseases; Hypertension
National Heart, Lung, and Blood Institute (NHLBI)
1984-06 PHASE3
NCT00267657 UNKNOWN
Amphetamine-Related Disorders
National Institute on Drug Abuse (NIDA)
2004-01 PHASE1

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