Meptazinol Hydrochloride - CAS 59263-76-2
Catalog number:
59263-76-2
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C15H23NO.HCl
Molecular Weight:
269.81
COA:
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Targets:
Opioid Receptor
Description:
Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]-dihydromorphine binding with IC50 of 58 nM.
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Purity:
>98%
MSDS:
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1.Determination of a novel carbamate AChE inhibitor meserine in mouse plasma, brain and rat plasma by LC-MS/MS: application to pharmacokinetic study after intravenous and subcutaneous administration.
Xie Y1, Jiang P1, Ge X1, Wang H2, Shao B1, Xie Q3, Qiu Z3, Chen H4. J Pharm Biomed Anal. 2014 Aug 5;96:156-61. doi: 10.1016/j.jpba.2014.03.025. Epub 2014 Mar 26.
In this paper a simple and sensitive method for determination of a novel phenylcarbamate AChE inhibitor, meserine, in mouse plasma, brain and rat plasma was evaluated using high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS). Separation was achieved on an Alltech Alltima-C18 column (150mm×2.1mm, 3μm, Deerfield, IL, USA) with isocratic elution at a flow rate of 0.35ml/min. Detection was performed under the multiple reaction monitoring (MRM) mode using an electrospray ionization (ESI) in the positive ion mode. The protein precipitation and liquid-liquid extraction methods were used for the pretreatment of plasma and brain homogenates, respectively. The calibration curves of meserine showed good linearity over the concentration range of 0.5-1000ng/ml for mouse and rat plasma and 0.5-500ng/ml for mouse brain. The intra- and inter-day precision were less than 9.34% and the accuracy was from 95.34% to 107.78% for QC samples.
2.Enantioseparation of meptazinol and its three intermediate enantiomers by capillary electrophoresis using a new cationic β-cyclodextrin derivative in single and dual cyclodextrin systems.
Yu J1, Zhao Y, Song J, Guo X. Biomed Chromatogr. 2014 Jun;28(6):868-74. doi: 10.1002/bmc.3187.
A new cationic β-cyclodextrin derivative, mono-6-deoxy-6-piperdine-β-cyclodextrin (PIP-β-CD), was synthesized and applied as a chiral selector for the enantioseparation of meptazinol and its three intermediate enantiomers (intermediates II-IV) in capillary electrophoresis. When PIP-β-CD was employed as the single CD system, intermediate II was baseline enantioseparated while the results for the other analytes were less satisfactory. In order to enhance the selectivity and resolution of meptazinol intermediate III and intermediate IV, dual CD systems of PIP-β-CD in combination with three different neutral CDs were synthesized and tested: β-cyclodextrin (β-CD), trimethyl-β-cyclodextrin (TM-β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD). After investigating the effect on the enantioseparation efficiency of the nature and the concentration of both CDs, the dual CD system consisting of PIP-β-CD and HP-β-CD was shown to be the most efficient for the simultaneous enantioseparation of meptazinol intermediates III and IV.
3.Must we press on until a young mother dies? Remifentanil patient controlled analgesia in labour may not be suited as a "poor man's epidural".
Kranke P1, Girard T, Lavand'homme P, Melber A, Jokinen J, Muellenbach RM, Wirbelauer J, Hönig A. BMC Pregnancy Childbirth. 2013 Jul 2;13:139. doi: 10.1186/1471-2393-13-139.
BACKGROUND: The epidural route is still considered the gold standard for labour analgesia, although it is not without serious consequences when incorrect placement goes unrecognized, e.g. in case of intravascular, intrathecal and subdural placements. Until now there has not been a viable alternative to epidural analgesia especially in view of the neonatal outcome and the need for respiratory support when long-acting opioids are used via the parenteral route. Pethidine and meptazinol are far from ideal having been described as providing rather sedation than analgesia, affecting the cardiotocograph (CTG), causing fetal acidosis and having active metabolites with prolonged half-lives especially in the neonate. Despite these obvious shortcomings, intramuscular and intravenously administered pethidine and comparable substances are still frequently used in delivery units. Since the end of the 90 ths remifentanil administered in a patient-controlled mode (PCA) had been reported as a useful alternative for labour analgesia in those women who either don't want, can't have or don't need epidural analgesia.
4.Enantiomeric separation of meptazinol and its three intermediate enantiomers by capillary electrophoresis: quantitative analysis of meptazinol in pharmaceutical formulations.
Yu J1, Jiang Z, Sun T, Ji F, Xu S, Wei L, Guo X. Biomed Chromatogr. 2014 Jan;28(1):135-41. doi: 10.1002/bmc.2997. Epub 2013 Jul 25.
A new capillary electrophoresis (CE) method using carboxymethyl-β-cyclodextrin (CM-β-CD) as chiral selector has been developed for the enantiomeric separation of meptazinol and its three intermediate enantiomers (intermediates II-IV), and validated for the application of quantitative determination of meptazinol in tablets. The primary factors affecting the separation efficiency, which include the chiral selector and its concentration, the buffer pH and composition, the organic modifiers used, and the applied voltage, were optimized. Baseline and satisfactory separations were obtained for meptazinol and its three intermediate enantiomers. For quantitative analysis of meptazinol, the method was performed at the condition using 2.0 mmol/L CM-β-CD in 20 mmol/L H3 PO4 buffer adjusted to a pH of 6.00 with an applied voltage of 15 kV and containing 5% acetonitrile. After validation of the method in terms of its linearity, limits of detection and quantitation, accuracy, precision and selectivity, the method was successfully applied to the quantitation of meptazinol in pharmaceutical formulations.
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CAS 59263-76-2 Meptazinol Hydrochloride

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