bluuebunny/crossref_metadata_2025_split huggingface dataset:
The calcium channel antagonist, verapamil, potentiates the inhibitory action of morphine on intestinal and biliary motility
Authors: Shah M H , Dikshit R K , Mansuri S M 
Published: April 2011

Abstract
The effects of morphine and verapamil have been assessed on the gastrointestinal propulsion of charcoal meal and egg yolk-induced gall bladder emptying in mice. Each drug significantly inhibited these functions. In combination, an additive effect was seen on the inhibition of gastrointestinal transit, whilst verapamil potentiated the morphine-induced inhibition of gall bladder emptying. It is concluded that calcium ion channel antagonists may potentiate the activity of opiate drugs.
High capacity for pulmonary first-pass elimination of propranolol in rats
Authors: Iwamoto Kikuo , Watanabe Jun , Aoyama Yoko 
Published: April 2011

Abstract
Plasma propranolol concentrations after i.v. and i.a. 1, 2&#x006d;̇5, 5 and 10 mg kg−1 doses of the drug given intravenously or intra-arterially have been compared in 7-week-old male Wistar rats. The areas under the curves after i.a. dosing were almost twice those after i.v. dosing at any dose, despite the elimination half-lives being the same. The difference in total body clearance after i.a. dosing from that after i.v. dosing indicated a significant contribution by pulmonary clearance, which ranged from about 20 to 30 mL min−1 kg−1, to the overall first-pass elimination after the i.v. administration. The pulmonary extraction ratio was approximately 0&#x006d;̇4 to 0&#x006d;̇5 at the i.v. doses used. Mean pulmonary transit time was estimated to be about 1 to 2 min. There was no dose-dependence in the pulmonary first-pass elimination kinetics of propranolol.
Punch velocities during the compaction process
Authors: Armstrong N Anthony , Palfrey Lynn P 
Published: April 2011

Abstract
Velocities achieved by the upper punch of an eccentric tablet press during compaction have been compared with those predicted by equations describing the movement of the punch in an empty die. Up to the point of maximum punch penetration, actual speeds are invariably less than the predicted speed, the magnitude of the deceleration being determined by the machine speed and applied force. As the punch withdraws from the die, its speed can exceed that predicted on theoretical grounds, due to the elastic expansion of the tablet assisting punch ejection.
Some aspects of the inhibitory activity of hypolaetin-8-glucoside in acute inflammation
Authors: Villar A , Gascó M A , Alcaraz M J 
Published: April 2011

Abstract
Hypolaetin-8-glucoside (H-8-G) has been examined for its mode of action in several models of acute inflammation. Its anti-inflammatory activity in carrageenan-induced inflammation of the rat hind-paw is not affected either by adrenalectomy or by phentolamine given with propranolol. H-8-G and its aglycone, hypolaetin, did not antagonize the actions of histamine, 5-hydroxytryptamine (5-HT), bradykinin or prostaglandin E2 (PGE2) on various smooth muscle preparations in-vitro, but protected erythrocytes from heat-induced lysis. The glycoside was more potent than troxerutin on capillary permeability increased by histamine and exerted inhibitory effects on protein exudation, leucocyte migration and β-glucuronidase activity in the carrageenan air pouch, thereby showing some difference from indomethacin. These results are discussed in relation to the features of non-steroidal anti-inflammatory drugs (NSAID) and flavonoid anti-inflammatory actions.
Effect of penetration enhancers on the permeation of mannitol, hydrocortisone and progesterone through human skin
Authors: Barry B W , Bennett S L 
Published: April 2011

Abstract
Mannitol, hydrocortisone and progesterone were selected as model penetrants to assess the mode of action of eight potential penetration enhancers in human skin. Their partition coefficients, octanol: water and stratum corneum: water were measured and correlated with their postulated routes of penetration through human skin. The results suggest that mannitol penetrated via a polar route, hydrocortisone by a mainly lipid route and progesterone via a lipid pathway but its penetration rate was probably affected by aqueous layers. From permeation studies through cadaver skin in which an in-vivo mimic method was used, it was concluded that the penetration enhancers fell into three main categories: (1) solvents which enhanced permeation of polar and non-polar compounds e.g. 2-pyrrolidone, N-methylpyrrolidone, N-methylformamide and propylene glycol plus Azone; (2) enhancers which preferentially affected the polar route e.g. propylene glycol plus decylmethylsulphoxide, and (3) accelerants which mainly modified the non-polar route e.g. propylene glycol plus oleic acid, propylene glycol alone and, to a limited extent, water.
Casting solvent effects on the permeability of polymer films of differing quaternary ammonium (cation) content
Authors: Okor R S , Anderson W 
Published: April 2011

Abstract
Films of certain acrylate-methacrylate copolymers of varying cation (quaternary ammonium) content were cast from three different solvents: acetone, chloroform, and ethanol; their permeability to urea was determined at 30 °C. In films containing 66 mole cation mol−1 polymer chain, and cast from acetone, chloroform or ethanol, the permeation rates were 480, 900 and 2807 mg h−1, respectively. Differences in permeation rates were however less significant when polymers of cation content lower than 46 mole cation mol−1 polymer chain were used to form films. This observation may relate to differences in the degree of dissociation of the polymer in the different solvents.
Fenfluramine antagonizes the stimulation of food intake induced by the putative 5-hydroxytryptamine1A agonist, isapirone, in non-fasted rats
Authors: Wong David T , Reid Leroy R 
Published: April 2011

Abstract
Isapirone, a 5-hydroxytryptamine1A receptor agonist, stimulated food intake in non-fasted rats in a dose-dependent manner (1, 3 and 10 mg kg−1 s.c). Fenfluramine, an antiobesity agent and a 5-HT releaser, at 3 and 10 mg kg−1 s.c. antagonized the isapirone-induced (3 mg kg−1 s.c.) feeding. These results are consistent with the known inhibitory role of 5-HT in the control of food intake in rats.
Direct vasomotor effects of theophylline and enprofylline on human coronary artery in-vitro: comparison with feline coronary and cerebral arteries
Authors: Sjögren Anders , Edvinsson Lars 
Published: April 2011

Abstract
The vasomotor effects of theophylline and enprofylline were investigated on circular segments of human coronary artery taken 6 h after death. Isolated arterial segments were examined using a sensitive myograph and isometric contractions were recorded with Grass transducers. The results were compared with those obtained in feline coronary and cerebral arteries. Theophylline and enprofylline induced pronounced relaxation of all types of precontracted arteries. In feline cerebral arteries the potency for eliciting relaxation was slightly higher for theophylline compared with enprofylline, while there was no difference in potency for the methylxanthines in coronary arteries. Prostaglandin F2α frequently induced rhythmic contractions in human, but not in feline coronary arteries. Theophylline increased the amplitude of the rhythmic contractions while this was not seen following administration of enprofylline. Whether this mode of activity by theophylline contributes to its arrhythmogenic properties in-situ requires clarification.
Mechanically strong films produced from cellulose acetate latexes
Authors: Bindschaedler C , Gurny R , Doelker E 
Published: April 2011

Abstract
Mechanically strong films, comparable with those obtained from organic solutions, can be produced from cellulose acetate latexes, a new type of dispersion, both by casting and spraying. The prerequisite conditions for high strength, which include choice of water-soluble plasticizers possessing some degree of volatility, are discussed.
The inhibition of monoamine oxidase by tricyclic antidepressants: the influence of the nature of the substrate and the source of the enzyme
Authors: Green A L , McGachy H Adrienne 
Published: April 2011

Abstract
Five tricyclic antidepressants, amitriptyline, clomipramine, desipramine, imipramine and iprindole, have comparable potencies as inhibitors of monoamine oxidase in rodent brain and liver. With rodent brain, potency was always greater with phenethylamine as substrate than with benzyl-amine, and was generally least with 5-HT. With mouse liver, in which monoamine oxidase is mainly B type, potency with tyramine and dopamine as substrates was close to that found with phenethylamine. The kinetics of inhibition varied with both the substrate and the tissue, and were inconsistent with a simple ping-pong model for substrate oxidation. The relevance of these observations to clinical effectiveness is discussed.
Pharmacokinetics and biliary excretion of rose bengal in rats with acute and chronic renal failure
Authors: Silberstein D J , Bowmer C J , Yates M S 
Published: April 2011

Abstract
The effects of glycerol-induced acute renal failure (ARF) and surgically induced chronic renal failure (CRF) on the pharmacokinetics and biliary excretion of rose bengal have been examined in the rat. Both the pharmacokinetics and biliary excretion of rose bengal were unaltered in either ARF or CRF. The latter results in CRF contrast with those of Tse et al (1976, Int. J. Nucl. Med. Biol. 3: 134–137) who reported decreased removal of the dye from blood and reduced biliary excretion. In addition, rose bengal behaves differently from bromosulphophthalein and indocyanine green whose hepatic uptake and initial biliary excretion are known to be decreased in ARF. The results suggest that rose bengal may have a hepato-biliary transport route which differs from that of bromosulphophthalein and indocyanine green, and the findings also emphasize the selective nature of altered organic anion uptake by the liver in ARF.
Effect of egg yolk lecithin on transdermal delivery of bunazosin hydrochloride
Authors: Kato Akira , Ishibashi Yasuo , Miyake Yasuo 
Published: April 2011

Abstract
Transdermal delivery of bunazosin HCl and the enhancing effect of egg yolk lecithin were examined using an in-vitro hairless mouse skin preparation and rabbits for in-vivo systemic absorption. The delivery of bunazosin in-vitro was small, but it was significantly enhanced when lecithin was incorporated into the same vehicle. This enhancing effect was confirmed with other drugs in-vitro. The enhancing ability was also seen in-vivo. Very little bunazosin was delivered from a propylene glycol suspension, but levels of 100–200 ng mL−1 were achieved by the incorporation of the lecithin.
Re-evaluation of the metabolism and excretion of diethylpropion in non-sustained and sustained release formulations
Authors: Beckett A H , Stanojčić Milena 
Published: April 2011

Abstract
A direct gas chromatographic method for unstable amino ketones, using a neutral column and moderately alkaline conditions during extraction has been developed. Its application has given a new perspective to the relative importance of the metabolic routes in the complex metabolism of diethylpropion which after oral administration in man is rapid and extensive (only 3–4% of the drug remains unchanged). Mono-N-de-ethylation is the main pathway (about 35% of the dose). N-De-ethylation is more important than carbonyl-reduction, occurring mainly with the unchanged drug (about 20% of the dose). Norephedrine, thought previously to be one of the main metabolites, has been shown to be present only in negligible amounts. About 30% of the dose, which cannot be accounted for as the sum of the amines recovered in urine, is probably metabolized by deamination, followed by oxidation and conjugation to give hippuric acid.
A comparative study of the interaction of warfarin with human α1-acid glycoprotein and human albumin
Authors: Otagiri M , Maruyama T , Imai T , Suenaga A , Imamura Y 
Published: April 2011

Abstract
The interaction of warfarin with human α1-acid glycoprotein (α1-AGP) and human albumin (HA) has been investigated using fluorescence and circular dichroism techniques. The fluorescence of warfarin is greatly enhanced following binding to α1-AGP or HA, the binding constant for a single site being estimated by the Scatchard method. The binding constants for the two serum proteins are similar, but the thermodynamic parameters differ. The binding constants increase as the pH is raised to 9&#x006d;̇0. Various basic drugs, such as chlorpromazine, propranolol and imipramine, markedly inhibited the binding of warfarin to α1-AGP. But, some acidic drugs, including phenylbutazone, effectively displaced warfarin bound to HA. The difference in CD spectra observed for α1-AGP and HA indicated that the drug-binding sites of the two proteins might have different asymmetries. It thus appears that the mode of interaction of warfarin with the two proteins differs.
Amiodarone and desethylamiodarone tissue uptake in rats chronically treated with amiodarone is non-linear with the dose
Authors: Latini R , Bizzi A , Cini M , Veneroni E , Marchi S , Riva E 
Published: April 2011

Abstract
Four groups of rats were given amiodarone chronically at 25, 37&#x006d;̇5, 50, 75 mg kg−1/12 h for 3 weeks; on day 21 the animals were killed and blood, plasma, heart, lung, liver and fat were collected and assayed for amiodarone and desethylamiodarone. Amiodarone plasma concentrations ranged from 0&#x006d;̇74 to 4&#x006d;̇68 μg mL−1 and desethylamiodarone from 0&#x006d;̇08 to 2&#x006d;̇05 μg mL−1. Plasma, blood and tissue concentrations of amiodarone and desethylamiodarone increased significantly with the dose. Blood/plasma and tissue/plasma partition ratios of amiodarone and desethylamiodarone increased significantly at the higher doses. Blood/plasma ratio was a good predictor of tissue/plasma ratios of amiodarone and its metabolite, except in fat. Total phospholipid concentrations in lung were correlated with amiodarone and desethylamiodarone concentrations in plasma, blood and lung.
The relation between effects of adenosine, theophylline and enprofylline on the contractility of sensitized guinea-pig lung strips
Authors: Napier Fiona E , Temple Diana M 
Published: April 2011

Abstract
Contractile responses of lung parenchymal strips from ovalbumin-sensitized guinea-pigs to cumulative addition of antigen were significantly potentiated by 10 min pretreatment with adenosine 10 μM. This potentiation was unaffected by the adenosine uptake inhibitor, dipyridamole, 2 μM. Cumulative addition of adenosine 0&#x006d;̇1–100 μM to parenchymal strips without antigen produced variable responses, unrelated to sensitization, some contracting, some relaxing. Theophylline 100 μM caused relaxation of parenchymal strips and significantly inhibited the antigen-induced contraction with a parallel shift of the log concentration-response line. It also inhibited the adenosine-induced potentiation of contraction. Enprofylline 100 μM caused a greater relaxation of the tissue than theophylline. While it inhibited the adenosine-induced potentiation of the response, enprofylline, in contrast to theophylline, failed to inhibit the antigen-induced contraction of guinea-pig parenchyma. At these concentrations, theophylline and enprofylline each inhibited the antigen-induced release of SRSA (leukotrienes C4, D4 and E4), and of histamine, from sensitized guinea-pig lung fragments.
Effects of magnesium chloride on the contractile response of uterus to several agonists in Ca-free solution
Authors: D'Ocon M P , Anselmi E , Villar A 
Published: April 2011

Abstract
The effects of MgCl2 on the oestrogen-dominated rat uterus have been examined. Tissues were preincubated in a Ca2+- and Mg2+-free medium containing 3 mM EDTA. Most experiments were subsequently performed in a similar medium containing either no EDTA or EDTA (1 mM). When MgCl2 was added cumulatively (1–32 mM) no contractile responses were obtained in Ca,Mg-free medium or in Ca,Mg-free high K+ solution. When 2 mM CaCl2 as added, a sustained contraction was obtained. Subsequent addition of cumulative concentrations of MgCl2 caused concentration-dependent relaxation. Oxytocin, 2 μM, produced a small and sustained contraction in a Ca,Mg-free medium. Addition of MgCl2, 2 mM, increased this contraction. In a Ca,Mg-free medium vanadate (8 times 10−5 M) did not evoke spasm of uterine smooth muscle. After addition of MgCl2 in cumulative amounts (1–32 mM) in the presence of vanadate, a concentration-dependent contraction was obtained. The present work shows that in Ca-free solution, maintained contractions induced by oxytocin and vanadate are augmented by Mg2+.
Extracts of feverfew may inhibit platelet behaviour via neutralization of sulphydryl groups
Authors: Heptinstall S , Groenewegen W A , Spangenberg P , Loesche W 
Published: April 2011

Abstract
It has been suggested that extracts of feverfew may inhibit platelet behaviour via effects on platelet sulphydryl groups. In the present study we have obtained evidence for such a mode of action. (i) Compounds that contain sulphydryl groups such as cysteine and N-(2-mercaptopropionyl)glycine prevented the inhibition of platelet behaviour by feverfew. (ii) Feverfew and parthenolide (one of the active components of feverfew) dramatically reduced the number of acid-soluble sulphydryl groups in platelets. This effect occurred at concentrations similar to those that inhibited platelet secretory activity. (iii) Feverfew itself did not induce the formation of disulphide-linked protein polymers in platelets but polymer formation occurred when aggregating agents were added to feverfew-treated platelets. (iv) Feverfew evoked changes in the metabolism of arachidonic acid that were similar to those observed in glutathione-depleted platelets.
The activity of compounds extracted from feverfew on histamine release from rat mast cells
Authors: Hayes N A , Foreman J C 
Published: April 2011

Abstract
An extract of the plant feverfew (Tanacetum parthenium) produces a dose-dependent inhibition of histamine release from rat peritoneal mast cells stimulated with anti-IgE or the calcium ionophore A23187. Greater inhibition of anti-IgE-induced histamine release was achieved with feverfew compared with the inhibition of A23187-induced release. Inhibition of anti-IgE-induced histamine release by feverfew extract was observed when the drug was added simultaneously with anti-IgE and the inhibitory activity increased only slightly when the drug was preincubated with the cells for 5 min before anti-IgE stimulation. In this respect feverfew differs from cromoglycate and quercetin. Feverfew extract inhibited anti-IgE-induced histamine release to the same extent in the absence and presence of extracellular glucose. It is concluded that feverfew extract contains a novel type of mast cell inhibitor.
Physicochemical investigations of dipolar aprotic solvents as potential cholelitholytic agents
Authors: Kennelly P , Corrigan O I 
Published: April 2011

Abstract
A number of dipolar aprotic solvents have been examined as potential co-solvents for gallstone dissolution. The power of these agents to solubilize such gallstone components as cholesterol, calcium carbonate, calcium palmi-tate and palmitic acid was determined and compared with that of monooctanoin (Capmul), using the synthetic solubility method. The solubilities of cholesterol and palmitic acid were greater in the N-methyl, N-ethyl and N-butyl-pyrrolidone derivatives than in monooctanoin. In contrast, the solubilities of the calcium salts were very low (&lt;0&#x006d;̇25% w/w) in all solvents examined. The influence of N-methylpyrrolidone (NMP) on both the in-vitro dissolution of cholesterol from gallstones and the decrease in stone weight with time was determined. NMP proved to be a better solvent than monooctanoin for human stones. NMP, which is miscible with water and monooctanoin, may have potential as a co-solvent in the design of solvent systems for gallstones.
Studies on thyrotropin-releasing hormone-induced micturition in cats
Authors: Beleslin Dušan B , Jovanović-Mićić Danica , Samardžić Ranka , Terzić Branka 
Published: April 2011

Abstract
In unanaesthetized cats micturition produced by thyrotropin-releasing hormone (TRH) was investigated after its injection into the cerebral ventricles through chronically implanted cannulae. TRH in doses from 0&#x006d;̇1 to 1&#x006d;̇0 mg evoked dose-dependent micturition. In cats treated with intracerebroventricular (i.c.v.) reserpine and 6-hydroxy-dopamine, but not with i.c.v. 5,6-dihydroxytryptamine and hemicholinium, the micturition caused by i.c.v. TRH was abolished. Chlorpromazine and antazoline injected into the cerebral ventricles prevented the micturition induced by i.c.v. TRH. On the other hand, mecamylamine, yohimbine, propranolol, atropine and methysergide injected i.c.v. had virtually no effect or partially antagonized the micturition evoked by TRH similarly injected. It is apparent therefore that centrally induced TRH micturition could be related to central catecholaminergic mechanisms.
Antiarrhythmic effect of desethylamiodarone in conscious rats
Authors: Varró András , Bódi Ilona , Rabloczky George 
Published: April 2011

Abstract
The effect of desethylamiodarone, a metabolite of amiodarone, was studied in the early phase of arrhythmias induced by coronary artery ligation in conscious rats. Desethylamiodarone pretreatment improved survival without altering the occurrence of different types of arrhythmias during the first 20 min after coronary ligation. It was concluded that desethylamiodarone may contribute to the antiarrhythmic effect seen after chronic amiodarone treatment.
The influence of drug sorption on pharmacokinetic studies of chlormethiazole and lignocaine
Authors: Upton Richard N , Mather Laurence E , Runciman William B 
Published: April 2011

Abstract
The influence of drug sorption on the measurement of dose and blood concentrations during pharmacokinetic studies of chlormethiazole and lignocaine in a chronically catheterized sheep preparation has been examined. There was no sorption to soda glass tubes, borosilicate glass volumetric flasks or soda glass microlitre syringes but minor sorption to polypropylene syringes, polypropylene pipette tips and rubber bottle stoppers after 240 min contact. During infusions through administration sets including either polyvinyl chloride or polyethylene catheters, no significant loss of lignocaine occurred, but only 41&#x006d;̇7–63&#x006d;̇9% of the chlormethiazole dose was delivered. No significant decreases in either drug occurred from blood sampled through an intravascular catheter and stopcock system. There was negligible degradation of the samples over 4 h. Sorption of chlormethiazole or lignocaine to the laboratory equipment used was not a significant source of error but polyvinyl chloride infusion catheters could result in significant reductions in chlormethiazole dose.
A gamma scintigraphic evaluation of the precorneal residence of liposomal formulations in the rabbit
Authors: Fitzgerald P , Hadgraft J , Wilson C G 
Published: April 2011

Abstract
Multilamellar liposomes were prepared from dipalmitoyl phosphatidylcholine or egg lecithin in combination with cholesterol and either dicetyl phosphate or stearylamine. The size and charge of the colloidal preparations were characterized before labelling with [111In]8-hydroxyquinoline. Freshly labelled liposomes were instilled into the eyes of unanaesthetized NZW rabbits and their disposition and drainage followed using gamma scintigraphy. A positive surface charge was found to affect significantly liposomal drainage rate, whereas an increase in size restricted drainage from the inner canthal region. Drainage of the suspending medium was directly compared with liposomes by labelling the medium with [99mTc] sodium pertechnetate and following the simultaneous change in removal of 99mTc and 111In from the precorneal area. Slower drainage rates were obtained for the suspending medium compared with solutions of the isotopes suggesting that the liposomes restricted solution drainage.