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NAP 226-90 Sale

(Synonyms: 3-(1-(S)-(N,N-二甲基氨基)乙基)苯酚) 目录号 : GC47746

A metabolite of rivastigmine

NAP 226-90 Chemical Structure

Cas No.:139306-10-8

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1 g
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25 g
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Sample solution is provided at 25 µL, 10mM.

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产品描述

NAP 226-90 is a metabolite of rivastigmine that is formed by hydrolysis.1

1.Polinsky, R.J.Clinical pharmacology of rivastigmine: A new-generation acetylcholinesterase inhibitor for the treatment of Alzheimer's diseaseClin. Ther.20(4)634-647(1998)

Chemical Properties

Cas No. 139306-10-8 SDF
别名 3-(1-(S)-(N,N-二甲基氨基)乙基)苯酚
Canonical SMILES OC1=CC=CC([C@@H](N(C)C)C)=C1
分子式 C10H15NO 分子量 165.2
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml 储存条件 Store at -20°C
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1 mM 6.0533 mL 30.2663 mL 60.5327 mL
5 mM 1.2107 mL 6.0533 mL 12.1065 mL
10 mM 0.6053 mL 3.0266 mL 6.0533 mL
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Research Update

Concentrations of rivastigmine and NAP 226-90 and the cognitive response in Taiwanese Alzheimer's disease patients

J Alzheimers Dis 2012;31(4):857-64.PMID:22751168DOI:10.3233/JAD-2012-120109.

The aim of this small pilot study was to evaluate the association between plasma concentrations of rivastigmine and its metabolite, NAP 226-90, and cognitive function in patients with Alzheimer's disease (AD). Rivastigmine-treated AD patients, who had been maintained on a fixed regimen of twice daily rivastigmine (6 to 12 mg/d) for ≥6 months, were eligible for evaluation. The assessments included cognitive assessment screening instrument (CASI) and clinical dementia rating scale, conducted at baseline and at 6-month follow-up. The 9 subdomains of CASI at baseline and follow-up were analyzed in relation to the plasma concentrations of rivastigmine and NAP 226-90, as measured by capillary electrophoresis. Logistic regression was performed to adjust for age, gender, education level, apolipoprotein E ε4 genotype status, and baseline CASI score to investigate the association between plasma rivastigmine and NAP 226-90 concentrations and the cognitive response. The total sample consisted of 53 clinically diagnosed AD patients taking rivastigmine only at doses of 6 mg to 9 mg/d because of intolerability at 12 mg/d. Higher rivastigmine concentration was significantly associated with improved or preserved short-term memory and worsened abstraction/judgment (p < 0.05), but not with changes in other domains (p > 0.05). Higher NAP 226-90 concentration was significantly associated with worsened abstraction/judgment (p < 0.05), but not with changes in other domains. Higher plasma rivastigmine concentration was significantly associated with improved or preserved short-term memory but worsened abstraction/judgment. An optimal concentration of rivastigmine should be quantified for each patient because of differential cognitive responses.

A simple, rapid and sensitive method for simultaneous determination of rivastigmine and its major metabolite NAP 226-90 in rat brain and plasma by reversed-phase liquid chromatography coupled to electrospray ionization mass spectrometry

Biomed Chromatogr 2004 Apr;18(3):160-6.PMID:15103701DOI:10.1002/bmc.304.

A simple and sensitive reversed-phase liquid chromatography coupled with electrospray-mass spectrometry was developed and validated for the simultaneous determination of rivastigmine, a cholinesterase inhibitor, and its major metabolite NAP 226-90 in rat plasma and brain homogenates. Rivastigmine and NAP 226-90 were extracted from plasma and brain by ethyl acetate and, after drying under nitrogen, re-dissolved in acetonitrile and separated isocratic by HPLC on a C(18) column and quantified by single ion monitoring mass spectrometer. The mean (+/-SD) extraction efficiency for rivastigmine in plasma and brain was 93 +/- 2 and 95 +/- 2% (n = 5) of NAP 226-90 in a drug range of 10-100 pmol/mL or pmol/g. The method proved to be linear within the tested range (regression coefficient, r = 0.9999, n = 5). Intra- and inter-day precision coefficients of variation and accuracy bias were acceptable (within 15%, n = 5) over the entire range for both compounds using plasma or brain samples. The limits of quantification were 0.5 pmol/mL plasma and 2.5 pmol/g brain for rivastigmine and 1 pmol/mL plasma and 5 pmol/g brain for NAP 226-90, respectively. The analytical technique was used to determine the concentrations of rivastigmine and its metabolite NAP 226-90 in rat plasma and brain after oral drug administration. The concentrations of the parent drug and its major metabolite were compared to a pharmacodynamic parameter, the ex vivo inhibition of acetylcholinesterase.

Simultaneous determination of galantamine, rivastigmine and NAP 226-90 in plasma by MEKC and its application in Alzheimer's disease

Electrophoresis 2009 Feb;30(4):644-53.PMID:19170055DOI:10.1002/elps.200800559.

A simple and sensitive MEKC with UV detection was developed and validated for the simultaneous determination of acetylcholinesterase inhibitors including galantamine, rivastigmine and major metabolite NAP 226-90 in plasma. A sample pretreatment by liquid-liquid extraction with diethylether and subsequent quantification by MEKC was used. The optimum separation for these analytes was achieved in <10 min at 25 degrees C with a fused-silica capillary column of 30.2 cm x 50 microm id (effective length 20 cm) and a run buffer containing 25 mM Tris buffer (pH 5.0) with 160 mM sodium octanesulfonate, 20% ACN and 0.01% PVP as a dynamic coating to reduce analytes' interaction with the capillary wall. For sensitivity consideration regarding the determination of linearity, LOD, quantitation and monitoring drugs concentration in patients, the detection wavelengths for galantamine or rivastigmine and NAP 226-90 were set at 214 or 200 nm, respectively. One male volunteer (26-year-old) was orally administered a single dose of 4.5 mg rivastigmine (Exelon, Novartis) in capsule, and blood samples were drawn over a 12 h period for concentration-time profile study. The method was also successfully applied for monitoring galantamine or rivastigmine and its metabolite NAP 226-90 in 11 Alzheimer's disease patients' plasma after oral administration of the commercial products Reminyl (8 mg galantamine/capsule) or Exelon (3 mg rivastigmine/capsule), respectively.

A simple and sensitive assay for the quantitative analysis of rivastigmine and its metabolite NAP 226-90 in human EDTA plasma using coupled liquid chromatography and tandem mass spectrometry

Rapid Commun Mass Spectrom 2006;20(22):3330-6.PMID:17044120DOI:10.1002/rcm.2737.

A sensitive and specific high-performance liquid chromatography/tandem mass spectrometry (HPLC/MS/MS) assay for the determination of rivastigmine and its major metabolite NAP 226-90 is presented. A 100 microL plasma aliquot was spiked with a structural analogue of rivastigmine as internal standard (PKF214-976-AE-1) and proteins were precipitated by adding 200 microL of methanol. After centrifugation a volume of 100 microL of the clear supernatant was mixed with 100 microL of methanol/water (30:70, v/v) and volumes of 25 microL were injected onto the HPLC system. Separation was acquired on a 150 x 2.0 mm i.d. Gemini C18 column using a gradient system with 10 mM ammonium hydroxide and methanol. Detection was performed by using a turboionspray interface and positive ion multiple reaction monitoring by tandem mass spectrometry. The assay quantifies rivastigmine from 0.25 to 50 ng/mL and its metabolite NAP 226-90 from 0.50 to 25 ng/mL, using human plasma samples of 100 microL. Validation results demonstrate that rivastigmine and metabolite concentrations can be accurately and precisely quantified in human EDTA plasma. This assay is now used to support clinical pharmacologic studies with rivastigmine.

Skinfold thickness for rivastigmine patch application in Alzheimer's disease

Psychopharmacology (Berl) 2019 Apr;236(4):1255-1260.PMID:30645680DOI:10.1007/s00213-018-5135-x.

Rationale: Rivastigmine patches are used for patients with Alzheimer's disease (AD), but little is known about the serum concentration of rivastigmine and its metabolite or clinical adherence in relation to skinfold thickness after rivastigmine patch application. Objectives: The aim of this study was to examine the association between rivastigmine and NAP 226-90 serum concentration and skinfold thickness and to determine the appropriate skinfold thickness for the use of rivastigmine patch in patients with AD. Methods: Patients with AD who continuously used rivastigmine patches (4.6 mg/24 h, 5 cm2) for more than 6 months were recruited. The serum concentrations of rivastigmine and NAP 226-90 were measured. Skinfold thickness was measured using a Lange Skinfold Caliper. Results: In total, 91 patients with AD (40 men and 51 women) participated in this study on skinfold thickness measurement. Among them, 27 patients were examined for rivastigmine and NAP 226-90 serum concentrations, with mean concentrations of 1.0 ± 0.6 ng/mL and 3.6 ± 3.6 ng/mL, respectively. The skinfold thickness in the subscapular area was significantly negatively correlated with the NAP 226-90 serum concentration (Spearman's rank correlation coefficient = - 0.47, P = .01). In addition, patients with AD and a subscapular skinfold thickness of ≥25 mm exhibited a significantly high risk of decreased Mini-Mental Status Examination score and nonadherence to a rivastigmine patch (odds ratio 3.00; 95% confidence interval = 1.076-8.366, P = .03). Conclusions: Subscapular skinfold thickness was significantly negatively correlated with the NAP 226-90 serum concentration and may be considered an appropriate predictor of response and adherence to clinical application of a rivastigmine patch.