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NG,NG-dimethyl-L-Arginine-d6 (hydrochloride)

(Synonyms: NG,NG-Dimethylarginine-d6 dihydrochloride) 目录号 : GC48837

An internal standard for the quantification of NG,NG-dimethyl-L-arginine

NG,NG-dimethyl-L-Arginine-d6 (hydrochloride) Chemical Structure

Cas No.:1313730-20-9

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NG,NG-dimethyl-L-arginine-d6 (ADMA-d6) (hydrochloride) is intended for use as an internal standard for the quantification of NG,NG-dimethyl-L-arginine by GC- or LC-MS. ADMA is an endogenous inhibitor of nitric oxide synthase (NOS).1,2 It is formed from arginine by protein arginine methyltransferases (PRMTs) and degraded by dimethylarginine dimethylaminohydrolases (DDAHs) and alanine-glyoxylate aminotransferase 2 (AGXT2).1 ADMA levels are increased concomitant with an increase in blood pressure in Dahl salt-sensitive rats fed a high-salt diet.2 ADMA levels are increased in the plasma in a variety of endothelial dysfunction-related diseases, including hypertension, congestive heart failure, and end-stage renal disease.1,3,4

1.Sydow, K., and MÜnzel, T.ADMA and oxidative stressAtheroscler. Suppl.4(4)41-51(2003) 2.Jin, J.S., and D'Alecy, L.G.Central and peripheral effects of asymmetric dimethylarginine, an endogenous nitric oxide synthetase inhibitorJ. Cardiovasc. Pharmacol.28(3)439-446(1996) 3.Vallance, P., Leone, A., Calver, A., et al.Accumulation of an endogenous inhibitor of nitric oxide synthesis in chronic renal failureLancet339(8793)572-575(1992) 4.Matsuoka, H., Itoh, S., Kimoto, M., et al.Asymmetrical dimethylarginine, an endogenous nitric oxide synthase inhibitor, in experimental hypertensionHypertension29(1 Pt 2)242-247(1997)

Chemical Properties

Cas No. 1313730-20-9 SDF
别名 NG,NG-Dimethylarginine-d6 dihydrochloride
Canonical SMILES [2H]C([2H])([2H])N(C([2H])([2H])[2H])C(NCCC[C@H](N)C(O)=O)=N.Cl.Cl
分子式 C8H12D6N4O2•2HCl 分子量 281.2
溶解度 DMF: 5 mg/ml,DMSO: 3 mg/ml,Ethanol: 3 mg/ml,PBS (pH 7.2): freely soluble 储存条件 -20°C; protect from light
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 3.5562 mL 17.7809 mL 35.5619 mL
5 mM 0.7112 mL 3.5562 mL 7.1124 mL
10 mM 0.3556 mL 1.7781 mL 3.5562 mL
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Research Update

Gateways to clinical trials

Methods Find Exp Clin Pharmacol 2004 Jan-Feb;26(1):53-84.PMID:14988742doi

Gateways to Clinical Trials is a guide to the most recent clinical trials in current literature and congresses. The data in the following tables has been retrieved from the Clinical Studies Knowledge Area of Prous Science Integrity, the drug discovery and development portal, http://integrity.prous.com. This issue focuses on the following selection of drugs: Abetimus sodium, Ad5-FGF4, adeno-Interferon gamma, AE-941, AERx, alemtuzumab, alicaforsen sodium, almotriptan, alpharadin, anakinra, anatumomab mafenatox, ANG-453, anti-CTLA-4 Mab, AP-12009, aprepitant, aripiprazole, arsenic trioxide, astemizole, atlizumab, atomoxetine hydrochloride; Bevacizumab, BG-9928, BMS-188667, botulinum toxin type B, BufferGel; Caffeine, CDP-870, cetuximab, cilomilast, ciluprevir, clofarabine, continuous erythropoiesis receptor activator, CP-461; Darbepoetin alfa, deferasirox, desloratadine, desoxyepothilone B, diflomotecan, dolasetron, drotrecogin alfa (activated), duloxetine hydrochloride; ED-71, efalizumab, efaproxiral sodium, EKB-569, eletriptan, EMD-72000, enfuvirtide, erlotinib hydrochloride, escitalopram oxalate, etoricoxib; Fampridine, ferumoxytol, fondaparinux sodium; Gadofosveset sodium, gastrazole, gefitinib, gemtuzumab ozogamicin, gepirone hydrochloride glutamine; hLM609, HSPPC-96, human insulin; IDD-1, imatinib mesylate, indisulam, inhaled insulin, ixabepilone; Keratinocyte growth factor; Lapatinib, laquinimod, LDP-02, LE-SN38, levetiracetam, levosimendan, licofelone, liposomal doxorubicin, liposomal NDDP, lopinavir, lumiracoxib, LY-156735; Morphine hydrochloride, morphine-6-glucuronide, motexafin gadolinium, MS-27-275, MVA-5T4, MVA-Muc1-IL-2; Nemifitide ditriflutate, neridronic acid nitronaproxen, NSC-683864, NSC-703940, NVP-LAF-237; Oblimersen sodium, ocinaplon, oncomyc-NG, OPC-28326, ortataxel, ospemifene; Palonosetron hydrochloride, PEG-filgrastim peginterferon alfa-2(a), peginterferon alfa-2b, pegsunercept, pemetrexed disodium, pregabalin, prilocaine, pyridoxamine; RDP-58, recombinant glucagon-like peptide-1 (7-36) amide, recombinant human ApoA-I milano/phospholipid complex; SB-715992, soblidotin, sodium dichloroacetate, St. John's Wort extract; TAS-102, terfenadine, TG-1024, TG-5001, 4'-Thio-ara-C, tipranavir, topixantrone hydrochloride, trabectedin, transdermal selegiline, trimethoprim, troxacitabine, TT-232; Vatalanib succinate, vinflunine; Ximelagatran; Ziprasidone hydrochloride, Zoledronic acid monohydrate.

Pharmaceuticals in two watersheds in Eastern China and their ecological risks

Environ Pollut 2021 May 15;277:116773.PMID:33640818DOI:10.1016/j.envpol.2021.116773.

Pharmaceuticals are of increasing environmental concern due to their potential threat to aquatic ecosystems. Intensive human activities are a major factor influencing the level of pharmaceutical pollution in aquatic ecosystems. In this study, we investigated the occurrence, ecological risks of 31 pharmaceuticals and the possible influence of human activities on pharmaceutical distribution in two watersheds in the Yangtze River Delta, Eastern China. The target compounds were grouped into six categories: three non-steroidal anti-inflammatory drugs, ten antibiotics, six cardiovascular drugs, five hormones, six psychotropic drugs, and one antiparasitic. All target pharmaceuticals were detected in the surface water samples, with dexamethasone (100% of samples), tetracycline (100% of samples), and cefradine (100% of samples) being the dominant compounds (maximum concentrations of 686, 128, and 2280 ng/L, respectively). The total pharmaceutical concentrations were significantly higher in the urban watershed (711-2790 ng/L, mean = 1150 ng/L) than in the peri-urban watershed (467-1525 ng/L, mean = 863 ng/L) (p < 0.05). Distinct variation in the total pharmaceutical concentration also occurred between the dry season (507-2790 ng/L, mean = 1100 ng/L) and the wet season (467-1525 ng/L, mean = 943 ng/L). Ecological risk assessment showed that in the two watersheds, benzylpenicillin potassium, tetracycline hydrochloride, chlormadinone, ampicillin, cefotaxime acid, atorvastatin, sertraline hydrochloride, and oxazepam posed a medium potential risk (0.1 < risk quotient < 1), while norethisterone posed a high potential risk (risk quotient > 1). Redundancy analysis revealed that the concentrations of pharmaceuticals in various categories were positively correlated with land-use type (urban and agricultural land-use percentages), population density, and distance from town in both watersheds. Urban and agricultural activities were likely the main factors influencing the concentrations and composition of pharmaceuticals in these aquatic environments. Positive correlations were also found between total pharmaceutical concentrations and population density in both watersheds, suggesting a significant contribution of human disturbance to pharmaceutical pollution. The results provide useful information for pharmaceutical pollution control, ecological risk assessment, and sustainable water management at the watershed scale.

Determination of pararosaniline hydrochloride in workplace air

Environ Monit Assess 2019 Jun 17;191(7):444.PMID:31209660DOI:10.1007/s10661-019-7568-z.

Pararosaniline hydrochloride (CPR) is a dye used for colouring paper, leather and natural and artificial fibres. It is also used in analytical and microbiological laboratories. It is a carcinogenic substance of category 1B. In analytical chemistry, it is used for detecting the following among others: bromates, formaldehyde, ozone, sulphite and sulfur dioxide. CPR is a dye commonly used in microbiology for staining preparations, for staining bacteria, antibodies or other organisms. In Poland, about 800 employees were exposed to this substance. The lack of methods for the determination of pararosaniline hydrochloride in workplace air makes it impossible to assess the occupational exposure of workers to this substance. For this reason, a determination method has been developed, which allows for the determination of pararosaniline hydrochloride in the air. This method makes it possible to determine the concentration of CPR in the air at the workplace within the range from 0.002 to 0.04 mg/m3 (for an air sample of 120 L). The method is based on the adsorption of pararosaniline hydrochloride present in the workplace air on a polypropylene filter, eluting the substance deposited on the filter with methanol and analysing the solution thus obtained using high-performance liquid chromatography with a diode array detector (wavelength of 544 nm). Using an Ultra C18 (250 mm length) chromatographic column at a temperature of 23 °C and the mobile phase of methanol:0.1% phosphoric acid(V) (95:5, v/v) at flow rate of 0.6 mL/min makes it possible to determine the content of pararosaniline hydrochloride in the presence of aniline, nitrobenzene and 4-tolylamine. Limit of detection and limit of quantification were 0.17 ng/mL and 0.51 ng/mL, respectively.

Compatibility of treprostinil sodium and dopamine hydrochloride during simulated Y-site administration

Am J Health Syst Pharm 2020 Apr 1;77(8):649-657.PMID:32236454DOI:10.1093/ajhp/zxaa025.

Purpose: To evaluate the physical and chemical compatibilities of treprostinil sodium and dopamine hydrochloride. Methods: Treprostinil sodium (4,000, 76,000, and 500,000 ng/mL) were mixed with dopamine hydrochloride (0.6, 3.2, 6, and 40 mg/mL). Samples were obtained at hours 0, 1, 2, and 4 for physical compatibility and chemical stability testing. Physical compatibility was assessed by visual examination and measurements of turbidity and pH. Drug concentrations were assessed using stability-indicating liquid chromatography mass spectrophotometry (LCMS) for treprostinil sodium and stability-indicating high-performance liquid chromatography (HPLC) for dopamine hydrochloride. Results: Treprostinil sodium 4,000 and 76,000 ng/mL, when mixed with dopamine hydrochloride 0.6, 3.2, 6, and 40 mg/mL, were stable for 4 hours. Treprostinil sodium 500,000 ng/mL was stable when mixed with dopamine hydrochloride 0.6 mg/mL for 4 hours, but when mixed with dopamine hydrochloride 3.2, 6, and 40 mg/mL, significant precipitation was seen. Conclusion: Treprostinil sodium 4,000 and 76,000 ng/mL were stable for 4 hours during simulated Y-site coadministration with dopamine hydrochloride 0.6, 3.2, 6, and 40 mg/mL. Treprostinil sodium 500,000 ng/mL is stable when mixed with dopamine hydrochloride 0.6 mg/mL.

Pharmacokinetic comparison of four arbidol hydrochloride preparations in beagle dogs

Biomed Chromatogr 2022 Jan;36(1):e5245.PMID:34532879DOI:10.1002/bmc.5245.

This study aimed to compare the pharmacokinetic properties of four preparations (dispersible tablets, ordinary tablets, capsules and granules) of arbidol hydrochloride, a broad-spectrum antiviral drug, in beagle dogs. Briefly, a single dose of 100 mg of the four preparations of arbidol hydrochloride was orally administered to dogs; blood was then collected from the veins of the foreleg at different times after administration to prepare plasma samples. The plasma concentration of arbidol hydrochloride was measured using a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS). The results showed that when orally administered with dispersible tablets, ordinary tablets, capsules and granules suspended with water, there were no significant differences in the pharmacokinetic parameters (including peak time, peak concentration, elimination half-life, area under the curve (AUC0-t ), and mean retention time) of arbidol hydrochloride. However, in the case of the dispersible tablets, the pharmacokinetics of arbidol hydrochloride was significantly affected by the mode of administration. Compared with direct feeding, peak time [0.50 (0.13, 0.50) vs. 1.00 (0.50, 2.00)] was significantly shortened (P = 0.033) and the AUC0-48 h (8726.5 ± 2509.3 vs. 3650.8 ± 1536.9 ng h/ml) was significantly increased (P = 0.012) when the dispersible tablets were orally administered as water dispersion. In conclusion, the pharmacokinetics of four preparations of arbidol hydrochloride were not significant different in beagle dogs. However, compared with direct feeding, the absorption of arbidol hydrochloride was faster and the bioavailability was better when the dispersible tablets were orally administered as water dispersion.