Inactivation of gamma-glutamylcysteine synthetase by SAPH-3 disulfide: role of the histaminyl moiety.


:Certain disulfide analogues of cystamine were prepared and evaluated for the ability to inhibit gamma-glutamylcysteine synthetase (GCS), the rate-limiting enzyme in glutathione synthesis. The compound SAPH-3 disulfide (2a) was found to be the most effective inactivator of GCS reported to date. Studies of structural analogues of 2a indicate that the histamine moiety plays a significant role in enzyme inactivation. Substitution of methyl groups on the carbon atoms adjacent to both sulfur atoms of the disulfide drastically decreases inhibitory action, probably due to a steric repulsion near the sulfur atom at the enzyme active site.


J Pharm Sci


Schor NF,Cheng B,Siuda JF




Has Abstract


1991-04-01 00:00:00














  • Chemical modification of hyaluronic acid for intraoral application.

    abstract::This study was aimed to investigate chemical preactivated thiomers for their potential use in mucosal drug delivery. Thiomers--thiolated polymers--are mucoadhesive polymers with sulfhydryl group-bearing side chains. Thiomers are synthesized by covalent attachment of low molecular mass compounds bearing sulfhydryl grou...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Laffleur F,Röggla J,Idrees MA,Griessinger J

    更新日期:2014-08-01 00:00:00

  • 1-(substituted benzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidones: a series with stimulant and depressant activities.

    abstract::A series of 1-(substituted benzyl)-3,4,5,6-tetrahydro-2(1H)-pyrimidones was synthesized primarily by catalytic hydrogenation of the corresponding 1-(substituted benzyl)-2(1H)-pyrimidone. The pharmacological evaluation of these compounds in mice revealed a unique profile that included evidence of CNS stimulation and de...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ellis KO,Schwan TJ,Wessels FL,Miles NJ

    更新日期:1980-10-01 00:00:00

  • Physico-chemical and technological properties of sodium naproxen granules prepared in a high-shear mixer-granulator.

    abstract::In the present work, authors produced tablets of anhydrous sodium naproxen by wet granulation using a high-shear mixer-granulator. Drug hydrated to the tetrahydrated form, as observed by X-ray powder diffractometry. After wet granulation, authors then performed two different drying procedures, obtaining granules of di...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Di Martino P,Malaj L,Censi R,Martelli S

    更新日期:2008-12-01 00:00:00

  • Simultaneous GLC determination of methyl salicylate and menthol in a topical analgesic formulation.

    abstract::A simultaneous GLC determination for methyl salicylate and menthol in a topical analgesic formulation is reported. n-Nonadecane is used as the internal standard. The method is rapid, accurate, precise, and selective in the presence of salicylic acid and ethyl salicylate. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Sapio JP,Sethachutkul K,Moody JE

    更新日期:1979-04-01 00:00:00

  • A Measurement and Modeling Study of Hair Partition of Neutral, Cationic, and Anionic Chemicals.

    abstract::Various neutral, cationic, and anionic chemicals contained in hair care products can be absorbed into hair fiber to modulate physicochemical properties such as color, strength, style, and volume. For environmental safety, there is also an interest in understanding hair absorption to wide chemical pollutants. There hav...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Li L,Yang S,Chen T,Han L,Lian G

    更新日期:2018-04-01 00:00:00

  • Assay and disposition of carvedilol enantiomers in humans and monkeys: evidence of stereoselective presystemic metabolism.

    abstract::Carvedilol is a new beta-blocking agent with vasodilating activities, which is a racemic mixture of R(+)- and S(-)-enantiomers. Since the two enantiomers differ in pharmacological properties, it is necessary to individually measure their plasma concentrations in order to evaluate the pharmacological effects of racemic...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Fujimaki M,Murakoshi Y,Hakusui H

    更新日期:1990-07-01 00:00:00

  • Suppository formulations as a potential treatment for nephropathic cystinosis.

    abstract::Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised lysosomal levels of cystine in the cells of all the organs. It is treated by the 6-h oral administration of the aminothiol, cysteamine, which has an offensive taste and smell. In an attempt to reduce this frequency and improve the tr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Buchan B,Kay G,Matthews KH,Cairns D

    更新日期:2012-10-01 00:00:00

  • Enhanced cytotoxicity of core modified chitosan based polymeric micelles for doxorubicin delivery.

    abstract::In this study, the cytotoxicity of doxorubicin (DOX) loaded stearic acid grafted chitosan oligosaccharide (CSO-SA) micelles and its core modified drug delivery systems were investigated in vitro. The in vitro drug release experiments using cellular culture medium, Roswell Park Memorial Institute 1640 (RPMI-1640) mediu...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ye YQ,Chen FY,Wu QA,Hu FQ,Du YZ,Yuan H,Yu HY

    更新日期:2009-02-01 00:00:00

  • Chloride ion nuclear magnetic resonance spectroscopy probe studies of copper and nickel binding to serum albumins.

    abstract::The binding of Cu2+ and Ni2+ to bovine, dog, and human serum albumin has been studied by the 35Cl NMR probe technique. The number of primary copper sites were estimated to be 1.3 for human serum albumin, 3.1 for bovine serum albumin, and 6.6 for dog serum albumin. A similar number of primary nickel sites was determine...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Mohanakrishnan P,Chignell CF,Cox RH

    更新日期:1985-01-01 00:00:00

  • Verification and validation of computational models used in biopharmaceutical manufacturing: Potential application of the ASME Verification and Validation 40 standard and FDA proposed AI/ML model life cycle management framework.

    abstract::A wide variety of computational models covering statistical, mechanistic, and machine learning (locked and adaptive) methods are explored for use in biopharmaceutical manufacturing. Limited discussion exists on how to establish the credibility of a computational model for application in biopharmaceutical manufacturing...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bideault G,Scaccia A,Zahel T,Forero RL,Daluwatte C

    更新日期:2021-01-22 00:00:00

  • New approaches for the preparation of hydrophobic heparin derivatives.

    abstract::A heparin derivative sufficiently lipophilic to be bound to plastics, forming blood-compatible supports, or to be used as an anticoagulant by transdermal or oral routes would be of great pharmaceutical interest. For such applications, the functional groups within heparin's antithrombin III binding site, responsible fo...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Liu J,Pervin A,Gallo CM,Desai UR,Van Gorp CL,Linhardt RJ

    更新日期:1994-07-01 00:00:00

  • Prediction of solubility in nonideal multicomponent systems using the UNIFAC group contribution model.

    abstract::There is a need to identify suitable blends of solvents to dissolve drugs. Empirical approaches, such as trial-and-error and response surface, require several solubility measurements. In this study the UNIFAC method was used to predict solubility in highly nonideal multicomponent systems in which only the solute entha...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ochsner AB,Sokoloski TD

    更新日期:1985-06-01 00:00:00

  • The Organic Anion-Transporting Peptide 2B1 Is Localized in the Basolateral Membrane of the Human Jejunum and Caco-2 Monolayers.

    abstract::The organic anion-transporting polypeptide (OATP) 2B1 which is ubiquitously expressed in the human body is assumed to play an important role in the cellular uptake of many drugs. Although the expression and function of this solute carrier transporter is well characterized in the human liver and other tissues, little i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Keiser M,Kaltheuner L,Wildberg C,Müller J,Grube M,Partecke LI,Heidecke CD,Oswald S

    更新日期:2017-09-01 00:00:00

  • Prediction of onset of crystallization from experimental relaxation times. II. Comparison between predicted and experimental onset times.

    abstract:UNLABELLED:Given a good correlation between onsets of crystallization and mobility above T(g), one might be able to predict crystallization onsets at a temperature of interest far below T(g) from this correlation and measurement of mobility at a temperature below T(g). Such predictions require that: (a) correlation bet...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Bhugra C,Shmeis R,Krill SL,Pikal MJ

    更新日期:2008-01-01 00:00:00

  • Three-Dimensional Printing of Carbamazepine Sustained-Release Scaffold.

    abstract::Carbamazepine is the first-line anti-epileptic drug for focal seizures and generalized tonic-clonic seizures. Although sustained-release formulations exist, an initial burst of drug release is still present and this results in side effects. Zero-order release formulations reduce fluctuations in serum drug concentratio...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Lim SH,Chia SM,Kang L,Yap KY

    更新日期:2016-07-01 00:00:00

  • Dissolution, stability, and absorption characteristics of dicumarol in polyethylene glycol 4000 solid dispersions.

    abstract::The dissolution characteristics of dicumarol were markedly enhanced by preparing dispersions of drug in polyethylene glycol 4000. Solid dispersions of varying weight fractions were formed by a melt method without measurable drug degradation or evaporation. There were no significant differences in dissolution rates amo...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Ravis WR,Chen CY

    更新日期:1981-12-01 00:00:00

  • Study of morphology of reactive dissolution interface using fractal geometry.

    abstract::The determination of reactive fractal dimension was carried out using two forms of the Noyes-Whitney equation, -dQ/dt = K(Q/Q0)DR/3 and -dQ/dt = K'RDR-3 using the Richardson plot on the basis of previous data obtained by dissolution of an orthoboric acid powder. The correlation of the results provided by the two ways ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tromelin A,Gnanou JC,Andrès C,Pourcelot Y,Chaillot B

    更新日期:1996-09-01 00:00:00

  • Pharmacokinetics of the antirheumatic proquazone in healthy humans.

    abstract::The pharmacokinetics of the antirheumatic proquazone and its conjugated and unconjugated m-hydroxy metabolites were investigated in five healthy male volunteers after both intravenous (75 and 122 mg) and peroral (300 and 900 mg via capsules) administration. For adequate intravenous dosing of the poorly water-soluble p...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Hinderling PH,Roos A

    更新日期:1984-03-01 00:00:00

  • Fluorescence assay of nitrofurantoin with o-aminothiophenol in plasma and urine.

    abstract::A fluorescence method is presented for the determination of nitrofurantoin based on conversion of the drug to a fluorescent substance. The method requires 0.1-0.5 ml of plasma or diluted urine and is 10 times more sensitive than the commonly used colorimetric method. ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Watari N,Funaki T,Kaneniwa N

    更新日期:1980-01-01 00:00:00

  • Effects of taraxacum mongolicum on the bioavailability and disposition of ciprofloxacin in rats.

    abstract::Taraxacum mongolicum (TM), also known as dandelion, is a herb widely used in the East for its antibacterial activity. The high mineral content of TM presents a potential problem for the absorption of quinolone antibiotics. This study was undertaken to discern the significance of a drug-drug interaction between TM and ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Zhu M,Wong PY,Li RC

    更新日期:1999-06-01 00:00:00

  • The Introduction of a New Flexible In Vivo Predictive Dissolution Apparatus, GIS-Alpha (GIS-α), to Study Dissolution Profiles of BCS Class IIb Drugs, Dipyridamole and Ketoconazole.

    abstract::The physiological pH changes and peristalsis activities in gastrointestinal (GI) tract have big impact on the dissolution of oral drug products, when those oral drug products include APIs with pH-dependent solubility. It is well documented that predicting the bioperformance of those oral drug products can be challengi...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Tsume Y,Patel S,Wang M,Hermans A,Kesisoglou F

    更新日期:2020-11-01 00:00:00

  • Stability of tetrahydrocannabinols II.

    abstract::The biphasic degradation of delta9-tetrahydrocannabinol (I), as monitored by flame-ionization GLC, produced delta8-tetrahydrocannabinol (II), cannabidiol (X), 9-hydroxyhexahydrocannabinol (VI), 9,10-dihydro-9-hydroxyisocannabidiol (VI), and and 6,12-dihydro-6-hydroxycannabidiol (VIII) in acidic solutions. Further iden...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Garrett ER,Gouyette AJ,Roseboom H

    更新日期:1978-01-01 00:00:00

  • Synthesis and antimicrobial activity of novel quinazolone derivatives.

    abstract::Three novel series of 4-oxoquinazoline derivatives were prepared and evaluated as potential antimicrobial agents. Evaluation of the antimicrobial activity of a variety of 4-substituted-1-thiosemicarbazides, 3,4-disubstituted thiazolines, and 3-substituted-5-thiazolidones reveals that the majority possess significant i...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Habib NS,Khalil MA

    更新日期:1984-07-01 00:00:00

  • The biologic effects of growth factor-toxin conjugates in models of vascular injury depend on dose, mode of delivery, and animal species.

    abstract::Toxin-conjugates, complexes designed from the fusion of tissue toxins and pathology-specific ligands, offer the potential for targeted cytotoxic therapy. Some have postulated that the recurrent failure of these conjugates to exhibit benefit in animal models of vascular injury arose because the timing and frequency of ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Yu C,Cunningham M,Rogers C,Dinbergs ID,Edelman ER

    更新日期:1998-11-01 00:00:00

  • Bioavailability of seocalcitol I: Relating solubility in biorelevant media with oral bioavailability in rats--effect of medium and long chain triglycerides.

    abstract::Simulated intestinal media (SIM) containing bile salt (BS) and phospholipids (PL) with and without medium chain lipolytic products (MC-LP) or long chain lipolytic products (LC-LP) were developed to study the solubility of seocalcitol. Both MC-LP and LC-LP were studied in order to investigate the influence of fatty aci...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Grove M,Pedersen GP,Nielsen JL,Müllertz A

    更新日期:2005-08-01 00:00:00

  • Isolation of 19alpha-H-lupeol from Maclura pomifera.

    abstract::A reinvestigation of the constituents of the Osage orange (maclura pomifera) yielded, in addition to the previously reported triterpenses (lupeol, butyrospermol, and lupan-3beta,20-diol), the pigments osajin and pomiferin, and a previously unreported constituent. The structure of this new compound was investigated. On...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Gearien JE,Klein M

    更新日期:1975-01-01 00:00:00

  • Drugs-biomolecule interactions: binding study of substrate and inhibitors to acetylcholinesterase using NMR.

    abstract::NMR was used to study the binding of acetylcholine, atropine, and physostigmine to acetylcholinesterase. Changes in the linewidth of the N-methyl resonance of acetylcholine, resulting from association with the enzyme during hydrolysis, were utilized to study the enzyme-substrate interaction. Physostigmine inhibited th...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Kato G

    更新日期:1975-03-01 00:00:00

  • Miscibility studies of indomethacin and Eudragit® E PO by thermal, rheological, and spectroscopic analysis.

    abstract::The objective of this study is to understand the underlying mechanisms responsible for the superior stability of indomethacin (INM)-Eudragit® E PO (E PO) system by exploring the miscibility and intermolecular interactions through the combination of thermal, rheological, and spectroscopic analysis. The zero shear-rate ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Liu H,Zhang X,Suwardie H,Wang P,Gogos CG

    更新日期:2012-06-01 00:00:00

  • Ditiocarb: decomposition in aqueous solution and effect of the volatile product on its pharmacological use.

    abstract::The kinetic profile for the decomposition of ditiocarb sodium salt in aqueous solution was achieved with UV-visible absorption spectrometry. The kinetic profile indicates that the decomposition reaction is hydrogen ion-catalyzed over the entire 4-10 pH range and enables the determination of the value of the acid-base ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Martens T,Langevin-Bermond D,Fleury MB

    更新日期:1993-04-01 00:00:00

  • Reevaluation of the absorption of carbenoxolone using an in situ rat intestinal technique.

    abstract::The absorption of the model drug carbenoxolone was reevaluated using an in situ rat intestinal perfusion technique in which disappearance from the intestinal lumen, binding to the perfused jejunal segment, and appearance in the mesenteric (jejunal) vein were measured. The effect of the degree of ionization on these pr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章


    authors: Blanchard J,Tang LM,Earle ME

    更新日期:1990-05-01 00:00:00