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Desoxypeganine

CAS# 495-59-0

Desoxypeganine

Catalog No. BCN8032----Order now to get a substantial discount!

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Quality Control of Desoxypeganine

Number of papers citing our products

Chemical structure

Desoxypeganine

3D structure

Chemical Properties of Desoxypeganine

Cas No. 495-59-0 SDF Download SDF
PubChem ID 442894 Appearance Powder
Formula C11H12N2 M.Wt 172.23
Type of Compound Alkaloids Storage Desiccate at -20°C
Solubility Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
Chemical Name 1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline
SMILES C1CC2=NC3=CC=CC=C3CN2C1
Standard InChIKey WUFQLZTXIWKION-UHFFFAOYSA-N
Standard InChI InChI=1S/C11H12N2/c1-2-5-10-9(4-1)8-13-7-3-6-11(13)12-10/h1-2,4-5H,3,6-8H2
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Source of Desoxypeganine

The herbs of Peganum harmala

Biological Activity of Desoxypeganine

Description1. Desoxypeganine is being developed for its potential utility in the pharmacological treatment of alcohol abuse to reduce craving and depression in alcohol abusers, and might also be useful as a smoking cessation aid. 2. Desoxypeganine is a cholinesterase inhibitor, acting preferentially on butyrylcholinesterase, and as a selective inhibitor of monoamine oxidase A but not monoamine oxidase B.
TargetsMAO

Desoxypeganine Dilution Calculator

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Desoxypeganine Molarity Calculator

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Preparing Stock Solutions of Desoxypeganine

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 5.8062 mL 29.0309 mL 58.0619 mL 116.1238 mL 145.1547 mL
5 mM 1.1612 mL 5.8062 mL 11.6124 mL 23.2248 mL 29.0309 mL
10 mM 0.5806 mL 2.9031 mL 5.8062 mL 11.6124 mL 14.5155 mL
50 mM 0.1161 mL 0.5806 mL 1.1612 mL 2.3225 mL 2.9031 mL
100 mM 0.0581 mL 0.2903 mL 0.5806 mL 1.1612 mL 1.4515 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Desoxypeganine

Phase I clinical trial with desoxypeganine, a new cholinesterase and selective MAO-A inhibitor: tolerance and pharmacokinetics study of escalating single oral doses.[Pubmed:18560630]

Methods Find Exp Clin Pharmacol. 2008 Mar;30(2):141-7.

Desoxypeganine (DOP) is a natural alkaloid that has been characterized as a cholinesterase inhibitor and a selective inhibitor of monoamine oxidase A. DOP has been investigated for its potential utility in the pharmacological treatment of alcohol abuse and as a smoking cessation aid. The aim of this clinical trial was to evaluate the tolerance and single-dose pharmacokinetic profile of DOP in healthy human volunteers. The study was an open-label, dose-escalation, phase I clinical trial involving the administration of increasing single oral doses of DOP (50, 100, 150 and 200 mg). The study was conducted according to the Declaration of Helsinki and Good Clinical Practice. Eighteen healthy adult volunteers (8 males and 10 females, age ranging 20-30 years) were recruited. DOP was administered sequentially, escalating in single doses of 50, 100, 150 and 200 mg in four experimental sessions with a washout period of at least 1 week between them. Progress to the next dose was allowed only if the previous dose was tolerated. Pharmacokinetic parameters were determined using noncompartmental methods. Clinical and analytical safety was assessed throughout the study, and QTc intervals were measured at regular intervals. The main pharmacokinetic parameters and renal excretion are described. No serious adverse events were registered, and none of the subjects discontinued the study because of lack of tolerance. All the adverse events recorded were mild to moderate and increased with the dose. The ECG measurements revealed that even at a higher dose, the QTc interval remained below the safety threshold. In summary, this first phase I study indicates that DOP has linear and dose-proportional pharmacokinetics, satisfactory oral bioavailability and plasma half-life and renal excretion. Also, DOP has shown an adequate safety profile that allows the continuation of clinical development.

Randomized, crossover, single-blind, placebo-controlled, human pharmacology clinical trial with desoxypeganine, a new cholinesterase and selective MAO-A inhibitor: multiple-dose pharmacokinetics.[Pubmed:19640356]

Int J Clin Pharmacol Ther. 2009 Jul;47(7):483-90.

UNLABELLED: Desoxypeganine, a naturally occurring alkaloid, is being developed for its potential utility in the pharmacological treatment of alcohol abuse to reduce craving and depression in alcohol abusers, and might also be useful as a smoking cessation aid. During the preclinical development it was characterized as a cholinesterase inhibitor, acting preferentially on butyrylcholinesterase, and as a selective inhibitor of monoamine oxidase A but not monoamine oxidase B. OBJECTIVE: The aim of the present human pharmacology clinical trial was to assess the oral bioavailability, pharmacokinetic profile and tolerability of Desoxypeganine, administered in a multiple-dose regimen to healthy volunteers. SUBJECTS AND METHODS: Eighteen healthy adult volunteers of both sexes received placebo, 50 mg and 100 mg Desoxypeganine (b.i.d. for 3 days) in a single-blind, crossover, randomized manner. Main pharmacokinetic parameters after single and multiple doses were estimated. Clinical tolerability and clinical laboratory safety, including effect on QTc interval, were assessed. RESULTS: Non-compartmental estimations of Cmax, AUC, tmax, t1/2 and MRT at 12-h intervals are given. No significant dose effect was observed in tmax, t1/2 and MRT. Cmax and AUC are approximately double with the dose of 100 mg comparing with the dose of 50 mg. A significant increase (p < 0.05) on Cmax and AUC was also obtained with the highest dose administered in comparison with the lowest one, revealing a slight but clinically insignificant accumulation. Steady state of drug concentration was reached in both genders during the study period. Plasma protein binding of Desoxypeganine amounted to approximately 18%. No severe adverse events were recorded and none of the subjects suffered from any adverse event that led to withdrawal from the study. Most frequently recorded adverse event was dizziness. No significant effects of Desoxypeganine on vital signs, laboratory parameters or QTc interval were observed. CONCLUSIONS: The present clinical trial describes the pharmacokinetic profile of two doses of Desoxypeganine, administered orally in multiple dose to healthy volunteers. The drug was well tolerated without any severe clinical, clinical laboratory, or ECG adverse events being recorded.

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