Renin inhibitor: transport mechanism in rat small intestinal brush-border membrane vesicles.

Abstract:

:The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The uptake of CH3-18 was markedly stimulated by an inwardly directed H+ gradient (pH 7.5 inside, pH 5.5 outside) and showed an uphill transport. It was competitively inhibited by tripeptides and tetrapeptides, but not by amino acids or dipeptides. A countertransport effect on the uptake of CH3-18 was observed in the vesicle preloaded with a tripeptide. Effects of the fragments of several renin inhibitors were evaluated by their inhibitory and countertransport effects on the uptake of CH3-18. The morpholino group at the N-terminal was found to be important for the uptake of CH3-18.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Hashimoto N,Fujioka T,Toyoda T,Muranushi N,Hirano K

doi

10.1023/a:1018900124257

subject

Has Abstract

pub_date

1994-10-01 00:00:00

pages

1448-51

issue

10

eissn

0724-8741

issn

1573-904X

journal_volume

11

pub_type

杂志文章
  • Immunopotentiator-Loaded Polymeric Microparticles as Robust Adjuvant to Improve Vaccine Efficacy.

    abstract:PURPOSE:Adjuvants are required to ensure the efficacy of subunit vaccines. Incorporating molecular immunopotentiators within particles could overcome drawbacks of molecular adjuvants (such as solubility and toxicity), and improve adjuvanticity of particles, achieving stronger adjuvant activity. Aim of this study is to ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1666-6

    authors: Zhang W,Wang L,Yang T,Liu Y,Chen X,Liu Q,Jia J,Ma G

    更新日期:2015-09-01 00:00:00

  • In situ intestinal absorption of a poorly water-soluble drug from mixed micellar solutions of bile salt and lipolysis products in rats.

    abstract::The role of a bile salt (sodium taurocholate) and lipolysis products (monoglyceride and fatty acid) in the intestinal absorption of a poorly water-soluble drug, diazepam, was investigated. Absorption rates and bioavailabilities were determined with the in situ rat gut technique of Doluisio et al. and analyzing the dia...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/A:1016312827680

    authors: Serajuddin AT,Rosoff M,Goldberg AH

    更新日期:1985-09-01 00:00:00

  • Selective adhesion of nanoparticles to inflamed tissue in gastric ulcers.

    abstract:PURPOSE:Gastrointestinal deposition of nanoparticles was examined after oral administration to mice suffering from an experimental gastric ulcer model. Local drug delivery could reduce side effects and would be a distinct improvement compared to existing therapeutic approaches, e.g. in the local therapy of Helicobacter...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-009-9834-1

    authors: Hassani S,Pellequer Y,Lamprecht A

    更新日期:2009-05-01 00:00:00

  • Development of Thiolated-Graphene Quantum Dots for Regulation of ROS in macrophages.

    abstract:PURPOSE:The current study was designed to develop thiolated-graphene quantum dots (SH-GQDs) as a theranostic nanocarrier and evaluate its potential for the optimal scavenging of reactive oxygen species (ROS) in macrophages. METHODS:SH-GQDs were prepared by hydrothermal pyrolysis of carbon source (citric acid) in the p...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-016-2000-7

    authors: Oh B,Lee CH

    更新日期:2016-11-01 00:00:00

  • Pharmacokinetics of methylergometrine in the rat: evidence for enterohepatic recirculation by a linked-rat model.

    abstract::The pharmacokinetics of methylergometrine were investigated in the rat, with emphasis on the role of biliary excretion and enterohepatic recirculation in the overall disposition of the drug. A linked-rat model, where the bile from a rat receiving a constant rate of iv infusion of methylergometrine was allowed to flow ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015871122537

    authors: Bredberg U,Paalzow L

    更新日期:1990-01-01 00:00:00

  • A simple rheological method for the in vitro assessment of mucin-polymer bioadhesive bond strength.

    abstract::A simple viscometric method was used to quantify mucin-polymer bioadhesive bond strength. Viscosities of 15% (w/v) porcine gastric mucin dispersions in 0.1 N HCl (pH 1) or 0.1 N acetate buffer (pH 5.5) were measured with a Brookfield viscometer in the absence (eta m) or presence (eta t) of selected neutral, anionic, a...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015812615635

    authors: Hassan EE,Gallo JM

    更新日期:1990-05-01 00:00:00

  • Comparison of CYP2D6 content and metoprolol oxidation between microsomes isolated from human livers and small intestines.

    abstract:PURPOSE:To assess the role of intestinal CYP2D6 in oral first-pass drug clearance by comparing the enzyme content and catalytic activity of a prototype CYP2D6 substrate, metoprolol, between microsomes prepared from human intestinal mucosa and from human livers. METHODS:Microsomes were prepared from a panel of 31 human...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018989211864

    authors: Madani S,Paine MF,Lewis L,Thummel KE,Shen DD

    更新日期:1999-08-01 00:00:00

  • Protamine sulfate enhances the transduction efficiency of recombinant adeno-associated virus-mediated gene delivery.

    abstract:PURPOSE:The purpose of this study was to evaluate glucose responsiveness in HepG2 human hepatoma cells transduced by a recombinant adeno-associated virus (rAAV) vector containing the insulin gene promoter. and to investigate the effect of protamine sulfate on rAAV-mediated gene delivery. METHODS:Recombinant AAV vector...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1010923924844

    authors: Yang YW,Hsieh YC

    更新日期:2001-07-01 00:00:00

  • Route of administration and sex differences in the pharmacokinetics of aspirin, administered as its lysine salt.

    abstract::One thousand milligrams of aspirin, as its lysine salt was administered intravenously, orally, and intramuscularly to nine male and nine female young healthy adult volunteers. After intravenous injection mean (+/- SD) values of clearance, steady-state volume of distribution, and terminal half-life were 12.2 +/- 2.2 ml...

    journal_title:Pharmaceutical research

    pub_type: 临床试验,杂志文章

    doi:10.1023/a:1015978104017

    authors: Aarons L,Hopkins K,Rowland M,Brossel S,Thiercelin JF

    更新日期:1989-08-01 00:00:00

  • A photo-activated targeting chemotherapy using glutathione sensitive camptothecin-loaded polymeric micelles.

    abstract:PURPOSE:A novel photo-activated targeted chemotherapy was developed by photochemical internalization (PCI) of glutathione-sensitive polymeric micelles incorporating camptothecin (CPT) prepared from thiolated CPT (CPT-DP) and thiolated poly(ethylene glycol)-b-poly(glutamic acid) (PEG-b-P(Glu-DP)) METHODS: PEG-b-P(Glu-DP...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-008-9712-2

    authors: Cabral H,Nakanishi M,Kumagai M,Jang WD,Nishiyama N,Kataoka K

    更新日期:2009-01-01 00:00:00

  • Osmotic-driven release kinetics of bioactive therapeutic proteins from a biodegradable elastomer are linear, constant, similar, and adjustable.

    abstract:PURPOSE:The aim of the study is to determine whether a biodegradable elastomeric device that uses an osmotic pressure delivery mechanism can release different therapeutic proteins at a nearly constant rate in nanomolar concentrations with high bioactivity, given the same formulation conditions. Vascular endothelial gro...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-006-9750-6

    authors: Gu F,Neufeld R,Amsden B

    更新日期:2006-04-01 00:00:00

  • The association of prescription status, patient age, patient gender, and patient question asking behavior with the content of pharmacist-patient communication.

    abstract:PURPOSE AND METHODS:Data from 358 pharmacist-patient encounters in 12 community pharmacies were used to investigate the association of prescription status, patient age, patient gender, and patient question asking with the content of pharmacist-patient communication. RESULTS:There was an association between prescriptio...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1012084207399

    authors: Schommer JC,Wiederholt JB

    更新日期:1997-02-01 00:00:00

  • Bioavailability prediction based on molecular structure for a diverse series of drugs.

    abstract:PURPOSE:Radial basis function artificial neural networks and theoretical descriptors were used to develop a quantitative structure-pharmacokinetic relationship for structurally diverse drug compounds. METHODS:Human bioavailability values were taken from the literature and descriptors were generated from the drug struc...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/b:pham.0000012154.09631.26

    authors: Turner JV,Maddalena DJ,Agatonovic-Kustrin S

    更新日期:2004-01-01 00:00:00

  • The Impact of Inadequate Temperature Storage Conditions on Aggregate and Particle Formation in Drugs Containing Tumor Necrosis Factor-Alpha Inhibitors.

    abstract:PURPOSE:To measure aggregate and particle formation in tumor necrosis factor-alpha (TNF-α) inhibitors etanercept, adalimumab and certolizumab pegol product samples after exposure to freezing temperature conditions similar to storage conditions previously observed in patients' homes. METHODS:TNF-α inhibitors in their o...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-017-2341-x

    authors: Vlieland ND,Nejadnik MR,Gardarsdottir H,Romeijn S,Sediq AS,Bouvy ML,Egberts ACG,van den Bemt BJF,Jiskoot W

    更新日期:2018-02-05 00:00:00

  • Supramolecular Chitosan Micro-Platelets Synergistically Enhance Anti-Candida albicans Activity of Amphotericin B Using an Immunocompetent Murine Model.

    abstract:PURPOSE:The aim of this work is to design new chitosan conjugates able to self-organize in aqueous solution in the form of micrometer-size platelets. When mixed with amphotericin B deoxycholate (AmB-DOC), micro-platelets act as a drug booster allowing further improvement in AmB-DOC anti-Candida albicans activity. METH...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-017-2117-3

    authors: Grisin T,Bories C,Bombardi M,Loiseau PM,Rouffiac V,Solgadi A,Mallet JM,Ponchel G,Bouchemal K

    更新日期:2017-05-01 00:00:00

  • Biodistribution and Toxicity of X-Ray Iodinated Contrast Agent in Nano-emulsions in Function of Their Size.

    abstract:PURPOSE:This study aimed to investigate the impact of the size of X-ray iodinated contrast agent in nano-emulsions, on their toxicity and fate in vivo. METHODS:A new compound, triiodobenzoate cholecalciferol, was synthetized, formulated as nano-emulsions, and followed after i.v. administration in mice by X-ray imaging...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1813-0

    authors: Attia MF,Anton N,Akasov R,Chiper M,Markvicheva E,Vandamme TF

    更新日期:2016-03-01 00:00:00

  • Synthesis, physicochemical properties, and cytotoxicity of a series of 5'-ester prodrugs of 5-iodo-2'-deoxyuridine.

    abstract::Five aliphatic 5'-esters of 5-iodo-2'deoxyuridine (IDU) were synthesized via an acid chloride alcoholysis reaction. The solubility in pH 7.4 phosphate buffer, lipophilicity as determined by partition experiments in octanol/pH 7.4 buffer, and cytotoxicity of these potential prodrugs were evaluated. The esters showed a ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015968113838

    authors: Narurkar MM,Mitra AK

    更新日期:1988-11-01 00:00:00

  • Long-acting atypical antipsychotics: characterization of the local tissue response.

    abstract:PURPOSE:Long-acting injectables (LAIs) are increasingly recognized as an effective therapeutic approach for treating chronic conditions. Many LAIs are formulated to create a poorly soluble depot from which the active agent is delivered over time. This long residing depot can cause localized chronic-active inflammation ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1308-4

    authors: Paquette SM,Dawit H,Hickey MB,Merisko-Liversidge E,Almarsson O,Deaver DR

    更新日期:2014-08-01 00:00:00

  • Anticancer drug-loaded nanospheres based on biodegradable amphiphilic ε-caprolactone and carbonate copolymers.

    abstract:PURPOSE:The aim was to investigate anticancer drug-loaded poly(carbonate-ester) nanospheres as potential drug delivery systems for cancer therapy. METHODS:Functional poly(carbonate-ester) copolymers (HPCP-SD) were synthesized by the incorporation of sulfadiazine as the tumor-targeting groups to hydroxyl groups of poly...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-010-0275-7

    authors: Yan GP,Zong RF,Li L,Fu T,Liu F,Yu XH

    更新日期:2010-12-01 00:00:00

  • In vitro Pharmacokinetic Cell Culture System that Simulates Physiologic Drug and Nanoparticle Exposure to Macrophages.

    abstract:PURPOSE:An in vitro dynamic pharmacokinetic (PK) cell culture system was developed to more precisely simulate physiologic nanoparticle/drug exposure. METHODS:A dynamic PK cell culture system was developed to more closely reflect physiologic nanoparticle/drug concentrations that are changing with time. Macrophages were...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-019-2576-9

    authors: Kutscher HL,Morse GD,Prasad PN,Reynolds JL

    更新日期:2019-02-01 00:00:00

  • Curcumin Delivery by Poly(Lactide)-Based Co-Polymeric Micelles: An In Vitro Anticancer Study.

    abstract:PURPOSE:This work describes the synthesis of block co-polymeric micelles, methoxy-poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA) to encapsulate Curcumin (CUR), thereby improving the dispersibility and chemical stability of curcumin, prolonging its cellular uptake and enhancing its bioavailability. METHODS:CUR-mPEG...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-015-1830-z

    authors: Kumari P,Swami MO,Nadipalli SK,Myneni S,Ghosh B,Biswas S

    更新日期:2016-04-01 00:00:00

  • An in vitro/in vivo correlation for the disintegration and onset of drug release from enteric-coated pellets.

    abstract::An empirical mass-transfer model for enteric-coating dissolution that uses in vivo dissolution data to characterize the pH-dependent solubility properties of the polymer film and a mass-transfer coefficient determined from in vivo dissolution or disintegration studies is developed. Once the in vivo mass-transfer coeff...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018986827350

    authors: Ebel JP,Jay M,Beihn RM

    更新日期:1993-02-01 00:00:00

  • Stereoselective dissolution of propranolol hydrochloride from hydroxypropyl methylcellulose matrices.

    abstract::Since many chiral pharmaceutical excipients, such as cellulose polymers and cyclodextrins, are used as stationary phases for the separation of enantiomers by high performance liquid chromatography (HPLC), it is hypothesized that one enantiomer of a chiral drug will be released faster than the other from a pharmaceutic...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018937123058

    authors: Duddu SP,Vakilynejad M,Jamali F,Grant DJ

    更新日期:1993-11-01 00:00:00

  • Enhanced delivery of 5-iodo-2'-deoxyuridine to the brain parenchyma.

    abstract::5'-Ester derivatives of 5-iodo-2'-deoxyuridine (IDU) with varying degrees of lipophilicity were examined to evaluate the effectiveness of lipophilic ester prodrugs for enhanced and sustained delivery of IDU to the brain parenchyma. Approximately 1.0% (1.0 +/- 0.19; n = 4) of the total radioactivity was found in the br...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015803922401

    authors: Ghosh MK,Mitra AK

    更新日期:1992-09-01 00:00:00

  • Hyaluronan-based nanocarriers with CD44-overexpressed cancer cell targeting.

    abstract:PURPOSE:The objective of the work was to evaluate the potential of hyaluronan-based nanoparticles as tumor-targeting nano-systems for CD44-overexpressed cancer therapy. METHODS:The synthesized amphiphilic cholesteryl succinoyl hyaluronan (Chol-Suc-HA) conjugates self-assembled into docetaxel(DTX)-loaded nanoparticles ...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-014-1393-4

    authors: Song S,Qi H,Xu J,Guo P,Chen F,Li F,Yang X,Sheng N,Wu Y,Pan W

    更新日期:2014-11-01 00:00:00

  • Hollow fibers as an oral sustained-release delivery system using propranolol hydrochloride.

    abstract::Fibers were spun by the downward configuration of the wet spinning technique. This configuration is capable of encapsulating nonspherical and/or coarse particles. We examined encapsulation of propranolol hydrochloride and the ability of the fibers to act as a sustained-release delivery system for propranolol hydrochlo...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1015982521706

    authors: Hussain MA,DiLuccio RC,Shefter E,Hurwitz AR

    更新日期:1989-12-01 00:00:00

  • Mechanism of the solution oxidation of rofecoxib under alkaline conditions.

    abstract:PURPOSE:The rapid oxidation of rofecoxib under alkaline conditions has been previously reported. The oxidation was reported to involve gamma-lactone ring opening to an alcohol, which further oxidized to a dicarboxyclic acid. The oxidation was suspected to be mediated by peroxy radicals. This work further investigates t...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-005-6947-z

    authors: Harmon PA,Biffar S,Pitzenberger SM,Reed RA

    更新日期:2005-10-01 00:00:00

  • Synergistic effect of formulated plasmid and needle-free injection for genetic vaccines.

    abstract:PURPOSE:A plasmid-based gene expression system was complexed with protective, interactive, and non-condensing (PINC) polymer system and administered with Medi-Jector, a needle-free injection device (NFID), to achieve high and sustained levels of antigen-specific antibodies in blood circulation. METHODS:Human growth ho...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1018834305079

    authors: Anwer K,Earle KA,Shi M,Wang J,Mumper RJ,Proctor B,Jansa K,Ledebur HC,Davis S,Eaglstein W,Rolland AP

    更新日期:1999-06-01 00:00:00

  • Effect of vehicles on the maximum transepidermal flux of similar size phenolic compounds.

    abstract:PURPOSE:In principle, maximum transepidermal fluxes of solutes should be similar for different vehicles, except when the solute or vehicle modifies the skin. Here we estimated maximum flux, stratum corneum solubility, diffusivity and permeability coefficient for a range of similarly sized phenolic compounds with varyin...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1007/s11095-012-0846-x

    authors: Zhang Q,Li P,Liu D,Roberts MS

    更新日期:2013-01-01 00:00:00

  • Possible role of anion exchanger AE2 as the intestinal monocarboxylic acid/anion antiporter.

    abstract:PURPOSE:The purpose of the present study was to investigate the transport of organic monocarboxylic acids mediated by the anion exchanger AE2, which has been already reported to be present at several tissue cell membranes, including intestinal brush border membrane in rabbit. METHODS:Membrane transport of organic mono...

    journal_title:Pharmaceutical research

    pub_type: 杂志文章

    doi:10.1023/a:1011920213991

    authors: Yabuuchi H,Tamai I,Sai Y,Tsuji A

    更新日期:1998-03-01 00:00:00