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Meclofenoxate hydrochloride

Drug for senile dementia and AD treatment CAS# 3685-84-5

Meclofenoxate hydrochloride

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Quality Control of Meclofenoxate hydrochloride

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Meclofenoxate hydrochloride

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Chemical Properties of Meclofenoxate hydrochloride

Cas No. 3685-84-5 SDF Download SDF
PubChem ID 19379 Appearance Powder
Formula C12H17Cl2NO3 M.Wt 294.17
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 50 mg/mL (169.97 mM)
H2O : 33.33 mg/mL (113.30 mM; Need ultrasonic)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-(dimethylamino)ethyl 2-(4-chlorophenoxy)acetate;hydrochloride
SMILES CN(C)CCOC(=O)COC1=CC=C(C=C1)Cl.Cl
Standard InChIKey FIVHOHCAXWQPGC-UHFFFAOYSA-N
Standard InChI InChI=1S/C12H16ClNO3.ClH/c1-14(2)7-8-16-12(15)9-17-11-5-3-10(13)4-6-11;/h3-6H,7-9H2,1-2H3;1H
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.

Biological Activity of Meclofenoxate hydrochloride

DescriptionMeclofenoxate hydrochloride, an ester of dimethylethanolamine (DMAE) and 4-chlorophenoxyacetic acid (pCPA), has been shown to improve memory, have a mentally stimulating effect, and improve general cognition. IC50 value: Target: nootropic Meclofenoxate, administered in a dose of 50 mg/kg twice daily for 7 days using the maze-training method, increased the number of responses to the conditioned stimulus, when retention tests were made 24 hours and 7 days after training, whereas citicholine, applied in the same way in a dose of 10 mg/kg, shortened the latency of the responses with reinforcement during the training and increased the number of correct responses to the conditioned stimulus in retention tests 7 days after the training [1]. Meclofenoxate appears to increase the consolidation of new information into long-term memory, but does not affect other aspects of remembering [2].

References:
[1]. Mosharrof AH, et al. Effects of meclofenoxate and citicholine on learning and memory in aged rats. Acta Physiol Pharmacol Bulg. 1987;13(4):17-24. [2]. Marcer D, et al. The differential effects of meclofenoxate on memory loss in the elderly. Age Ageing. 1977 May;6(2):123-31.

Meclofenoxate hydrochloride Dilution Calculator

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Preparing Stock Solutions of Meclofenoxate hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.3994 mL 16.997 mL 33.9939 mL 67.9879 mL 84.9849 mL
5 mM 0.6799 mL 3.3994 mL 6.7988 mL 13.5976 mL 16.997 mL
10 mM 0.3399 mL 1.6997 mL 3.3994 mL 6.7988 mL 8.4985 mL
50 mM 0.068 mL 0.3399 mL 0.6799 mL 1.3598 mL 1.6997 mL
100 mM 0.034 mL 0.17 mL 0.3399 mL 0.6799 mL 0.8498 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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Background on Meclofenoxate hydrochloride

Meclofenoxate hydrochloride, an ester of dimethylethanolamine (DMAE) and 4-chlorophenoxyacetic acid (pCPA), has been shown to improve memory, have a mentally stimulating effect, and improve general cognition.

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References on Meclofenoxate hydrochloride

Kinetics of hydrolysis of meclofenoxate hydrochloride in human plasma.[Pubmed:2883287]

J Pharm Pharmacol. 1987 Mar;39(3):215-8.

The kinetics of hydrolysis of Meclofenoxate hydrochloride in human plasma have been compared with those of clofibrate. The hydrolysis rate in fractionated plasma was determined in the presence and absence of a plasma esterase inhibitor, tetraethyl pyrophosphate. The kinetic data indicated that clofibrate decomposed only by esterase-induced hydrolysis, which was inhibited by binding of clofibrate to plasma proteins. In contrast to clofibrate, meclofenoxate decomposed rapidly in human plasma via spontaneous hydrolysis as well as esterase-induced hydrolysis. The spontaneous hydrolysis appeared to be inhibited by some components present in the esterase fraction isolated from plasma, while no significant inhibition of the hydrolysis by protein binding was observed.

Bioequivalence and pharmacokinetic comparison of a single 200-mg dose of meclofenoxate hydrochloride capsule and tablet formulations in healthy Chinese adult male volunteers: a randomized sequence, open-label, two-period crossover study.[Pubmed:18840370]

Clin Ther. 2008 Sep;30(9):1651-7.

BACKGROUND: Meclofenoxate hydrochloride is a psychostimulant in the nootropic agent group available in capsule and tablet formulations approved for traumatic cataphora, alcoholic poisoning, anoxia neonatorum, and children's enuresis in China. Although these 2 generic formulations are marketed in China, information regarding their pharmacokinetics and bioequivalence in humans has not been published. OBJECTIVE: The aim of this study was to compare the pharmacokinetic properties and bioequivalence of the capsule (test) and tablet (reference) formulations of Meclofenoxate hydrochloride 200 mg in healthy Chinese volunteers. METHODS: This single-dose, randomized-sequence, open-label, 2-period crossover study was performed at the Nanjing First Hospital of Nanjing Medical University, Nanjing, China. Eligible subjects were healthy male volunteers who were randomly assigned at a 1:1 ratio to receive a single 200-mg dose of the test or reference formulation, followed by a 1-week washout period and administration of the alternate formulation. The study drugs were administered after a 12-hour overnight fast. As a prodrug, meclofenoxate is hydrolyzed into 4-chlorophenoxyacetic acid and is not detected in plasma. The active metabolite of meclofenoxate, chlorophenoxyacetic acid, was assayed using a high-performance liquid chromatography method. For analysis of pharmacokinetic properties, including Cmax, AUC0-24, and AUC0-infinity, blood samples were obtained at 0.33, 0.67, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 14, and 24 hours after administration. The formulations were considered bioequivalent if the log-transformed ratios of Cmax and AUC were within the predetermined equivalence range (80%-125%) as established by the US Food and Drug Administration (FDA). Subjects were interviewed concerning the occurrence of adverse events including excitement, insomnia, lassitude, and headache. Tolerability was assessed at baseline (before administration) and at 1, 2, 6, and 12 hours after administration by monitoring vital signs and laboratory tests (hematology, blood biochemistry, hepatic function, and urinalysis). RESULTS: Twenty-four Chinese male subjects (mean [range]age,23.5[22-30]years;weight,63.3[56-68]kg; height, 171 [165-184] cm) were enrolled; all completed the study. No period or sequence effect was observed. The 90% CIs for the log-transformed ratios of chlorophenoxyacetic acid Cmax, AUC0-24, and AUC0-infinity were 95.7 to 122.9, 97.6 to 111.9, and 97.8 to 111.7, respectively (all, P>0.05). Similar results were found for the data without log-transformation. No adverse events were reported or observed during this single-dose study. CONCLUSIONS: In this small study in healthy Chinese adult male volunteers, a single 200-mg dose of the capsule formulation was found to be bioequivalent to a single 200-mg dose of the tablet formulation based on the US FDA's regulatory definition (rate and extent of absorption). Both formulations were well tolerated.

Construction and performance characteristics of new ion selective electrodes based on carbon nanotubes for determination of meclofenoxate hydrochloride.[Pubmed:22632051]

Anal Chim Acta. 2012 Jun 12;730:99-111.

This work offers construction and comparative evaluation the performance characteristics of conventional polymer (I), carbon paste (II) and carbon nanotubes chemically modified carbon paste ion selective electrodes (III) for Meclofenoxate hydrochloride are described. These electrodes depend mainly on the incorporation of the ion pair of Meclofenoxate hydrochloride with phosphomolybdic acid (PMA) or phosphotungestic acid (PTA). They showed near Nernestian responses over usable concentration range 1.0 x 10(-5) to 1.0 x 10(-2)M with slopes in the range 55.15-59.74 mV(concentrationdecade)(-1). These developed electrodes were fully characterized in terms of their composition, response time, working concentration range, life span, usable pH and temperature range. The electrodes showed a very good selectivity for Meclo with respect to a large number of inorganic cations, sugars and in the presence of the degradation product of the drug (p-chloro phenoxy acetic acid). The standard additions method was applied to the determination of MecloCl in pure solution, pharmaceutical preparations and biological samples. Dissolution testing was also applied using the proposed sensors.

Description

Meclofenoxate hydrochloride, an ester of dimethylethanolamine (DMAE) and 4-chlorophenoxyacetic acid (pCPA), has been shown to improve memory, have a mentally stimulating effect, and improve general cognition.

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