Indolizine derivatives with biological activity IV: 3-(2-Aminoethyl)-2-methylindolizine, 3-(2-aminoethyl)-2-methyl-5,6,7,8-tetrahydroindolizine, and their N-alkyl derivatives.

Abstract:

:In a continuing search for new biologically active agents derived from indolizine, 3-(2-aminoethyl)-2-methylindolizine, 3-(2-aminoethyl)-2-methyl-5,6,7,8-tetrahydroindolizine, and some mono- and di-N-substituted derivatives were prepared. Initial pharmacological screening showed that these compounds possess anti-5-hydroxytryptamine, antihistamine, antiacetylcholine, and CNS-depressant activities.

journal_name

J Pharm Sci

authors

Antonini I,Claudi F,Gulini U,Micossi L,Venturi F

doi

10.1002/jps.2600680317

subject

Has Abstract

pub_date

1979-03-01 00:00:00

pages

321-4

issue

3

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)42539-0

journal_volume

68

pub_type

杂志文章
  • Brain delivery of proteins by the intranasal route of administration: a comparison of cationic liposomes versus aqueous solution formulations.

    abstract::The goal of this research was to evaluate the effectiveness of cationic liposomes for intranasal administration of proteins to the brain. Cationic liposomes were loaded with a model protein, ovalbumin (OVAL), and a 50 microg dose was administered intranasally to rats. In qualitative studies, liposomes were loaded with...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21939

    authors: Migliore MM,Vyas TK,Campbell RB,Amiji MM,Waszczak BL

    更新日期:2010-04-01 00:00:00

  • Analytical methods for the determination of sulindac and metabolites in plasma, urine, bile, and gastric fluid by liquid chromatography using ultraviolet detection.

    abstract::A high-performance liquid chromatographic method using a linear elution gradient has been developed for the analysis of sulindac, sulindac sulfone, and sulindac sulfide in plasma, urine, bile, and gastric fluid. The methodology uses reverse-phase, radial compression chromatography with gradient elution, and UV detecti...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730921

    authors: Musson DG,Vincek WC,Constanzer ML,Detty TE

    更新日期:1984-09-01 00:00:00

  • Immunohistochemical localization of insulin-degrading enzyme along the rat intestine, in the human colon adenocarcinoma cell line (Caco-2), and in human ileum.

    abstract::Insulin-degrading enzyme (IDE) has been implicated in the intracellular degradation of insulin in insulin target cells. Knowledge of the existence of this enzyme in the intestine will be beneficial to the achievement of clinical oral efficacy of insulin. A comparative study was conducted with rat intestine, human colo...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js960035q

    authors: Chang LL,Stout LE,Wong WD,Buls JG,Rothenberger DA,Shier WT,Sorenson RL,Bai JP

    更新日期:1997-01-01 00:00:00

  • Impact of plasmid quality on lipoplex-mediated transfection.

    abstract::This work investigates the impact of quality attributes (impurity content, plasmid charge, and compactness) of plasmid DNA isolated with different purification methodologies on the characteristics of lipoplexes prepared thereof (size, zeta potential, stability) and on their ability to transfect mammalian cells. A 3.7 ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23709

    authors: De La Vega J,Braak BT,Azzoni AR,Monteiro GA,Prazeres DM

    更新日期:2013-11-01 00:00:00

  • Improved techniques for the photometric determination of partition coefficients, with particular reference to the chloroform-ammonia solvent system.

    abstract::Accurate partition coefficients K = Corg/Caq in chloroform-ammonia can be obtained by measuring the absorbance of the aqueous layer, replenishing with fresh aqueous solvent, and remeasuring the absorption after reequilibration. Provided the solute has a reasonably strong UV absorption, only 0.1-5 mg of material is req...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730222

    authors: Rummens FH,Bujaczek RF,Peters M,Green RD

    更新日期:1984-02-01 00:00:00

  • Econazole nitrate-loaded MCM-41 for an antifungal topical powder formulation.

    abstract::The aim of this article was to prepare a topical powder for the treatment of fungal infections, such as Candida intertrigo and tinea pedis. Thus, an econazole nitrate (ECO) formulation with improved drug dissolution and proper moisture adsorption was designed. ECO was melt with the mesoporous silicate MCM-41 (drug/MCM...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22183

    authors: Ambrogi V,Perioli L,Pagano C,Marmottini F,Moretti M,Mizzi F,Rossi C

    更新日期:2010-11-01 00:00:00

  • Improved burns therapy: liposomes-in-hydrogel delivery system for mupirocin.

    abstract::Wounds, particularly burns, are prone to colonization of potentially life-threatening bacteria. Local delivery of antimicrobial agents in sufficient quantities and over longer period of time can reduce risk of burn infections. Mupirocin-in-liposomes-in-hydrogels were proposed as advanced delivery system for improved b...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23260

    authors: Hurler J,Berg OA,Skar M,Conradi AH,Johnsen PJ,Skalko-Basnet N

    更新日期:2012-10-01 00:00:00

  • Paper chromatographic determination of chlortetracycline.

    abstract::Chlortetracycline was successfully separated from its degradation products and from other tetracyclines on a paper chromatogram previously impregnated with a mixture of edetate disodium and urea solution in pH 5.0 McIlvaine buffer. Chlortetracycline separation from its degradation products and from both tetracycline a...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600670432

    authors: Youssef MK,Attia IA,Safwat S

    更新日期:1978-04-01 00:00:00

  • Photodegradation of benzydamine: phototoxicity of an isolated photoproduct on erythrocytes.

    abstract::Benzydamine hydrochloride (Tantum, 1) is a photoallergic and phototoxic anti-inflammatory and analgesic agent. This drug is photolabile under aerobic and anaerobic conditions. Irradiation of a methanol solution of benzydamine under oxygen or argon at 300 nm affords 5-hydroxybenzydamine (2) and 2-beta-dimethylaminoprop...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600820407

    authors: Vargas F,Rivas C,Machado R,Sarabia Z

    更新日期:1993-04-01 00:00:00

  • Preparation and release characteristics of potassium chloride microcapsules.

    abstract::The release characteristics of potassium chloride was studied when it was coated with a selection of polymers; from the results obtained, a suitable batch was microencapsulated using a gelatin-gum arabic coacervate system. The microencapsulated product offers better controlled release for this drug when compared to st...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600700413

    authors: Harris MS

    更新日期:1981-04-01 00:00:00

  • Reaction of a peptide with polyvinylpyrrolidone in the solid state.

    abstract::During stability studies at high temperature (70 degrees C) and low relative humidity ( approximately 0%), the recovery of an asparagine containing hexapeptide (VYPNGA) and its known deamidation products from solid polyvinylpyrrolidone (PVP) matrices was incomplete. To determine the causes of this mass loss, formulati...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.10316

    authors: D'Souza AJ,Schowen RL,Borchardt RT,Salsbury JS,Munson EJ,Topp EM

    更新日期:2003-03-01 00:00:00

  • Specific interactions in high concentration antibody solutions resulting in high viscosity.

    abstract::The purpose of this work was to investigate the self-associating behavior observed in high concentration monoclonal antibody (MAb1) solutions at pH 6.0. Zeta potential measurements over the pH range (4.0-9.0) showed lower net charges present on the molecule at pH 6.0 and 7.0. The point of zero charge or crossover from...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21898

    authors: Yadav S,Liu J,Shire SJ,Kalonia DS

    更新日期:2010-03-01 00:00:00

  • Effect of bile salts on nasal permeability in vitro.

    abstract::Nasal mucosa excised from dogs or rabbits was mounted as a flat sheet in an in vitro chamber. The permeability was assessed by measuring the unidirectional flux of the radiolabeled tracer compounds, water, sucrose, polyethylene glycol, and cholecystokinin octapeptide. The permeability coefficients calculated from the ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600761206

    authors: Hersey SJ,Jackson RT

    更新日期:1987-12-01 00:00:00

  • Antitumor agents LV: Effects of genkwadaphnin and yuanhuacine on nucleic acid synthesis of P-388 lymphocytic leukemia cells.

    abstract::The diterpene esters, genkwadaphnin and yuanhuacine, have been shown to possess significant antileukemic activity in the P-388 screen. The major metabolic effects of the diterpene esters were on DNA and protein synthesis. The effects on DNA synthesis in vitro were evoked at a lower concentration than that required for...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600711120

    authors: Hall IH,Kasai R,Wu RY,Tagahara K,Lee KH

    更新日期:1982-11-01 00:00:00

  • Monitoring the film coating unit operation and predicting drug dissolution using terahertz pulsed imaging.

    abstract::Understanding the coating unit operation is imperative to improve product quality and reduce output risks for coated solid dosage forms. Three batches of sustained-release tablets coated with the same process parameters (pan speed, spray rate, etc.) were subjected to terahertz pulsed imaging (TPI) analysis followed by...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.21766

    authors: Ho L,Müller R,Gordon KC,Kleinebudde P,Pepper M,Rades T,Shen Y,Taday PF,Zeitler JA

    更新日期:2009-12-01 00:00:00

  • Liquid chromatographic analysis of dichlorophen and its major impurity.

    abstract::A rapid and simple high-performance liquid chromatographic (HPLC) method for the analysis of dichlorophen in raw material and in dichlorophen-toluene soft gelatin capsules for veterinary use was developed using a reverse-phase technique. This HPLC system was shown to isolate dichlorophen from its major impurity (the t...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730629

    authors: Shah KA,Samuels SA,Michaels MK,Warren JW

    更新日期:1984-06-01 00:00:00

  • Rate- and Extent-Limiting Factors of Oral Drug Absorption: Theory and Applications.

    abstract::The oral absorption of drugs has been represented by various concepts such as the absorption potential, the maximum absorbable dose, the biopharmaceutics classification system, and in vitro-in vivo correlation. The aim of this article is to provide an overview of the theoretical relationships between these concepts. I...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章,评审

    doi:10.1002/jps.24391

    authors: Sugano K,Terada K

    更新日期:2015-09-01 00:00:00

  • In Situ Lipolysis and Synchrotron Small-Angle X-ray Scattering for the Direct Determination of the Precipitation and Solid-State Form of a Poorly Water-Soluble Drug During Digestion of a Lipid-Based Formulation.

    abstract::In situ lipolysis and synchrotron small-angle X-ray scattering (SAXS) were used to directly detect and elucidate the solid-state form of precipitated fenofibrate from the digestion of a model lipid-based formulation (LBF). This method was developed in light of recent findings that indicate variability in solid-state f...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24634

    authors: Khan J,Hawley A,Rades T,Boyd BJ

    更新日期:2016-09-01 00:00:00

  • A novel off-center paddle impeller (OPI) dissolution testing system for reproducible dissolution testing of solid dosage forms.

    abstract::Dissolution testing is routinely conducted in the pharmaceutical industry to provide in vitro drug release information for quality control purposes. The most common dissolution testing system for solid dosage forms is the United States Pharmacopeia (USP) Dissolution Testing Apparatus 2. This apparatus is very sensitiv...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.22783

    authors: Wang Y,Armenante PM

    更新日期:2012-02-01 00:00:00

  • "Predicting" Polymorphs of Pharmaceuticals Using Hydrogen Bond Propensities: Probenecid and Its Two Single-Crystal-to-Single-Crystal Phase Transitions.

    abstract::The recently developed hydrogen-bonding propensity tool in the Cambridge Structural Database software package (Mercury) was tested to predict polymorphs. The compounds for the study were chosen from a list of approximately 300 pharmaceutically important compounds, for which multiple crystal forms had not been previous...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.24449

    authors: Nauha E,Bernstein J

    更新日期:2015-06-01 00:00:00

  • Preparation of insulin loaded PLGA-Hp55 nanoparticles for oral delivery.

    abstract::The aim of the present work was to investigate the preparation of PLGA nanoparticles (PNP) and PLGA-Hp55 nanoparticles (PHNP) as potential drug carriers for oral insulin delivery. The nanoparticles were prepared by a modified emulsion solvent diffusion method in water, and their physicochemical characteristics, drug r...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.20750

    authors: Cui FD,Tao AJ,Cun DM,Zhang LQ,Shi K

    更新日期:2007-02-01 00:00:00

  • Integrated functions for four basic models of indirect pharmacodynamic response.

    abstract::The integrated solutions (ABEC, area between baseline and effect curve) of four basic models of indirect pharmacodynamic responses are developed. These models assume that drug can inhibit or stimulate the production or loss of the response variable. For two models (I and III) with monoexponential drug disposition, exp...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1021/js970168r

    authors: Krzyzanski W,Jusko WJ

    更新日期:1998-01-01 00:00:00

  • Chemometric evaluation of brompheniramine-tannate complexes.

    abstract::The objective of the current study was to evaluate the performance of Raman and near-infrared (NIR) techniques combined with chemometrics in characterizing the critical quality attributes of brompheniramine (BP)-tannate complexes. Seven complexes were prepared and evaluated for chemical interactions, solubilities, dis...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23030

    authors: Zidan AS,Rahman Z,Khan MA

    更新日期:2012-04-01 00:00:00

  • In Vivo Performance of Fenofibrate Formulated With Ordered Mesoporous Silica Versus 2-Marketed Formulations: A Comparative Bioavailability Study in Beagle Dogs.

    abstract::The present study aims to evaluate the in vitro and in vivo performance of ordered mesoporous silica (OMS) as a carrier for the poorly water-soluble compound fenofibrate. Fenofibrate was loaded into OMS via incipient wetness impregnation to obtain a 29% drug load and formulated into capsules. Two capsule dosage forms ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2016.05.019

    authors: Bukara K,Schueller L,Rosier J,Daems T,Verheyden L,Eelen S,Martens JA,Van den Mooter G,Bugarski B,Kiekens F

    更新日期:2016-08-01 00:00:00

  • Combined Treatment of Tyrosine Kinase Inhibitor-Labeled Gold Nanorod Encapsulated Albumin With Laser Thermal Ablation in a Renal Cell Carcinoma Model.

    abstract::To characterize and evaluate human serum albumin-encapsulated nanoparticles for drug delivery of a tyrosine kinase inhibitor combined with induction of photothermal ablation combination therapy of renal cell carcinoma (RCC), nanoparticles of varying preparations and concentrations were characterized via zeta potential...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1016/j.xphs.2015.11.017

    authors: Callaghan C,Peralta D,Liu J,Mandava SH,Maddox M,Dash S,Tarr MA,Lee BR

    更新日期:2016-01-01 00:00:00

  • Diffusion and concentration profiles of drugs in gels.

    abstract::A versatile membraneless method was used to study the diffusion of acetaminophen, ibuprofen, indomethacin, theophylline, and chlorpheniramine in thermoreversible gels. Two independent ways to calculate the diffusion coefficients and to verify Fickian transport are presented; the most sensitive criterion for Fickian tr...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600821106

    authors: Upadrashta SM,Häglund BO,Sundelöf LO

    更新日期:1993-11-01 00:00:00

  • Long-term controlled navel administration of testosterone.

    abstract::Male fertility has reportedly been regulated by the long-term, continuous administration of testosterone. To deliver the testosterone at a controlled rate for a month or longer, a bandage-type, testosterone-releasing, disk-shaped device was developed. In vitro drug elution studies demonstrated that a constant release ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600730811

    authors: Chien YW

    更新日期:1984-08-01 00:00:00

  • A theoretical and experimental study of additive effects of physical aging and antiplasticization on the water permeability of polymer film coatings.

    abstract::The effects of physical aging and antiplasticization on the water transport properties of glassy cellulose acetate film-coated tablets were investigated. The gradual approach toward thermodynamic equilibrium during physical aging decrease the free volume of the polymers. This decrease in free volume is accompanied by ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600830337

    authors: Guo JH

    更新日期:1994-03-01 00:00:00

  • Intravenous dosing conditions may affect systemic clearance for highly lipophilic drugs: implications for lymphatic transport and absolute bioavailability studies.

    abstract::The clearance (Cl) and volume of distribution (V(ss)) of a lipophilic, lymphatically transported drug, halofantrine (Hf) have been evaluated after intravenous delivery to the systemic circulation in ex vivo lymph and plasma, and compared with the data obtained after administration of a lipid-based emulsion and a lipid...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.23211

    authors: Caliph SM,Trevaskis NL,Charman WN,Porter CJ

    更新日期:2012-09-01 00:00:00

  • Biodegradable microspheres. X: Some properties of polyacryl starch microparticles prepared from acrylic acid-esterified starch.

    abstract::Acrylic acid-esterified starch was produced by reacting starch with acrylic acid chloride. This reaction was rapid and easy to control. Introduction of acrylic groups into starch reduced the enzymatic degradability of starch (e.g., with 12 acrylic groups/100 glucose residues, approximately 75% of the degradation produ...

    journal_title:Journal of pharmaceutical sciences

    pub_type: 杂志文章

    doi:10.1002/jps.2600761219

    authors: Laakso T,Sjöholm I

    更新日期:1987-12-01 00:00:00