bluuebunny/crossref_metadata_2025_split huggingface dataset:
A method for stabilization of monoamine oxidases in homogenates of rat intestine epithelium
Authors: Barwell C J , Canham C A 
Published: April 2011

Abstract
In a homogenate of epithelium isolated from the small intestine of male Wistar rats, the amine oxidase activity with 10−3M tyramine was 9200 ± 200 nmol (g tissue)−1 h−1 of which 91% was due to the A form of monoamine oxidase (MAO) and 9% to the B form. Semicarbazide-sensitive amine oxidase activity was not detected with either 10−3M tyramine or 10−4M benzylamine as substrate. However, it was detectable in the homogenate of the gut residue where the activity with 10−4M benzylamine was 3600±200 nmol (g tissue)−1 h−1. The MAO activity, in homogenates of epithelium prepared with 0.1 M sodium phosphate pH 7.4, was stable at 4°C for at least 6 h whilst at minus 20°C it decreased by 70% within 24 h. Incorporation of 10% (v/v) glycerol into the homogenization medium stabilized the enzymes. The total activity and proportions due to MAO-A and MAO-B and kinetic constants for tyramine and 5-hydroxytryptamine, did not alter during 5 weeks storage at −20°C. The ability to store tissue homogenates should facilitate studies of intestinal amine oxidases.
The serum amyloid P response in the mouse air pouch
Authors: Bottomley K M K , Rising T J , Steward A 
Published: April 2011

Abstract
Levels of the acute phase reactant serum amyloid P (SAP) have been measured in the mouse pouch model of rheumatoid arthritis. Implantation of cartilage resulted in a significant and rapid elevation in the SAP concentration, which remained high for the duration of the experiment (14 days). Initial studies with several clinically employed antirheumatic drugs indicated that dexamethasone and cyclosporin A had a marked inhibitory effect.
Formation and In-vitro Evaluation of Theophylline-loaded Poly(methyl methacrylate) Microspheres
Authors: Pongpaibul Yanee , Maruyama Kazuo , Iwatsuru Motoharu 
Published: April 2011

Abstract
Theophylline-loaded poly(methyl methacrylate) (PMM) microspheres were prepared by the solvent evaporation method. Increasing the drug to polymer ratio increased both the mean particle size of the microspheres and the release rate. Polyethylene glycol (PEG) 4000 was used to improve the release rate of theophylline from the microspheres. No marked effect was observed on particle size distribution of the microspheres as a function of PEG concentration but there was a pronounced effect on drug release. The different particle sizes of microspheres prepared from the same drug to polymer ratio showed no significant difference in drug content, indicating that the ratio between theophylline and PMM remained practically constant regardless of the size of microspheres. Release characteristics of the microspheres were influenced by drug to polymer ratio, the amount of PEG incorporated and the particle size of microspheres. The release rate was slightly higher in simulated gastric fluid than in simulated intestinal fluid. The release profiles of the drug were modified by mixing microspheres of different formulations in different ratios.
Pharmacological profile of a chromanamine analogue (DP-6OH-3CA) of the selective presynaptic dopamine agonist N, N-dipropyl-7-hydroxy-2-aminotetralin
Authors: Vermue Niek A , Dukstra Durk , Horn Alan S 
Published: April 2011

Abstract
The pharmacological profile of an oxygen isostere of the selective presynaptic dopamine agonist DP-7OH-AT, i.e. dipropyl-6-hydroxy-3-chromanamine (DP-6OH-3CA) has been evaluated in various receptor binding, neurobiochemical and behavioural experiments. The chromanamine displaced the 3H-labelled dopamine ligands, 5,6-DPAT and N-0437, with Ki values of 106 and 143 nM, respectively. In in-vivo biochemical models for presynaptic activity the chromanamine induced a half-maximal effect in the γ-butyrolactone reversal test at 6.8 μmiol kg−1 and had an ED70 value of 40 μmol kg−1 for HVA decrease in the striatum. In behavioural models for postsynaptic dopaminergic activity a half-maximal effect for the induction of stereotypy was reached at 100 μmol kg−1 and reversal of the effects of reserpine to a level of 200 counts was induced at 11 μmol kg−1. On comparison of these results with the results obtained with the carbon analogue of DP-6OH-3CA, i.e. DP-7OH-AT, it is apparent that the chromanamine has a reduced potency for dopamine D2 receptors in in-vitro and in-vivo models. The selectivity for presynaptic dopamine receptors was lower than with DP-7OH-AT and the isomeric chromanamine, DP-8OH-3CA, indicating that the optimal position of the hydroxyl group for presynaptic selectivity is in the 8 and not in the 6 position for the chromanamines.
Enhancement of adenosine-induced relaxant responses of the guinea-pig isolated taenia coli and aortae by a novel nootropic agent BY-1949: comparison with dipyridamole
Authors: Tanabe Shigeru , Ikeda Yugo , Shiraki Yasuyuki , Sakal Kazushige 
Published: April 2011

Abstract
In muscle strips of guinea-pig taenia coli and aortae, the effects of 3-methoxy-1 1-methyldibenz[b,f][1,4]oxazepine-8-carboxylate (BY-1949) on the relaxant response to adenosine have been compared with those of dipyridamole. BY-1949 (3 × 10−5–10−4 M) as well as dipyridamole (3 × 10−7–10−5 M) resulted in a significant potentiation of relaxant responses to a cumulative administration of adenosine (10−6–10−3 M), but the drugs did not affect the response to noradrenaline and acetylcholine. The results indicate that BY-1949 exerts a selective potentiating effect on reactivity to exogenous adenosine.
Brain penetration of orally administered sodium pyroglutamate
Authors: Chanal J L , Audran M , Sicard M T , Briley M 
Published: April 2011

Abstract
The absorption and brain penetration of [3H]pyroglutamate was determined after oral administration to rats. Gas-liquid chromatography of the methylated derivatives followed by mass fragmentometry was used to analyse the plasma and brain levels of pyroglutamate. [3H]Pyroglutamate was separated from other labelled compounds by thin layer chromatography. The administration of 500 mg kg−1 [3H]pyroglutamate resulted in a 30-fold increase in plasma levels and a doubling in the brain levels. Over 60% of the cerebral radioactivity was present as [3H]pyroglutamate demonstrating that pyroglutamate is not only well absorbed but also penetrates in significant amounts into the brain.
Identification of 5-HT3 recognition sites in the ferret area postrema
Authors: Barnes N M , Costall B , Naylor R J , Tattersall F D 
Published: April 2011

Abstract
The 5-HT3 receptor antagonist [3H]zacopride was used to identify 5-HT3 recognition sites in the ferret area postrema. Specific binding was determined by the inclusion of the 5-HT3 receptor antagonist BRL 43694 in the incubation media, and was shown to be much higher in the area postrema than in other brain regions. The increased binding in the area postrema may reflect either a greater number of binding sites, a higher affinity for such sites, or both. The results indicate that 5-HT3 recognition sites are present within the area postrema and may afford an antiemetic site of action for zacopride and other 5-HT3 receptor antagonists.
The Effects of 1-Methyl-4-phenylpyridinium Ion (MPP+) on the Efflux and Metabolism of Endogenous Dopamine in Rat Striatal Slices
Authors: Snape B M , Pileblad E , Ekman A , Magnusson T , Carlsson A , Engel J 
Published: April 2011

Abstract
1-Methyl-4-phenylpyridinium ion (MPP+) was shown to accumulate concentration-dependently in slices from rat striatum. At 10 μM, MPP+, the tissue concentration was found to be 118 ± 9 μM following 75 min of incubation. The accumulation of MPP+ was reduced in the presence of 10 μM of the selective dopamine uptake inhibitor GBR 12909 (−50%) or by destruction of the dopaminergic terminals by complete hemisection of the forebrain 4 days before the experiments (−75%). Accumulation of MPP+ in the catecholamine-poor occipital cortex and cerebellum was only 25% of that obtained in striatum. Reserpine pretreatment of the rats in-vivo did not modify the accumulation of MPP+ in the striatal slices. MPP+ (1–10 μM) increased the net efflux of dopamine and reduced the efflux of the dopamine metabolite DOPAC from the striatal slices. The effect on dopamine was readily diminished if MPP+, after a 15 min incubation, was then omitted from the medium. In contrast, the DOPAC efflux was reduced for 75 min even though MPP+ was present in the incubation medium only for the first 15 min. In the presence of the monoamine oxidase inhibitor, pargyline (350 μM), MPP+ also produced an increase in dopamine efflux. In normal medium, the presence of the dopamine uptake inhibitor GBR 12909 (10 μM), or the absence of calcium, failed to modify the MPP+-induced increase in dopamine efflux. MPP+ also increased dopamine efflux from slices from reserpinized rats. In normal medium, MPP+ (10 μM) was much more effective than GBR 12909 (10 μM) in increasing dopamine efflux, whereas in the presence of pargyline both drugs were equally effective. It is suggested that, in rat striatal slices, MPP+ is selectively accumulated within the dopaminergic nerve terminals by means of a carrier mediated transport, sensitive to GBR 12909. It is concluded that MPP+ increases dopamine efflux largely by inhibiting monoamine oxidase and by inhibiting dopamine uptake. These data are discussed in relation to the previously observed action of MPTP on dopamine metabolism in mouse brain in-vivo.
Importance of D-2 Mechanisms in the Reversal of Reserpine Hypothermia in the Mouse
Authors: Volterra G , Borsini F , Meli A 
Published: April 2011

Abstract
The D-2 agonist LY 171555 (0.05, 0.1, 0.2 mg kg−1 s.c.) but not the D-1 agonist SK&F 38393 (5, 10, 20 mg kg−1 s.c.) reduced reserpine-induced hypothermia (RIH) in mice. This effect was antagonized by the D-2 antagonist (-)-sulpiride (50 mg kg−1 i.p.) but not by the D-1 antagonist SCH 23390 (0.1 mg kg−1 s.c). SK&F 38393 (20 and 1 mg kg−1 s.c.) did not alter the effect of LY 171555 (0.1 and 0.2 mg kg−1) on RIH, but administration of both LY 171555 (0.2 mg kg−1 s.c.) and SK&F 38393 (1 mg kg−1 s.c.) antagonized the reserpine-induced sedation.
Sustained release of indomethacin from chitosan granules in beagle dogs
Authors: Miyazaki Shozo , Yamaguchi Hideki , Yokouchi Chizuko , Takada Masahiko , Hou Wei-Min 
Published: April 2011

Abstract
The potential of chitosan granules as an oral sustained-release dosage form of indomethacin has been compared with conventional capsules in beagle dogs. When a commercial capsule was administered orally, the plasma concentrations reached the maximum level in 30 min. The granules did not give a sharp peak to the plasma concentration, but produced a sustained plateau of the drug. This may be due to the slow rate of release and a longer residence time in the stomach. Thus, in terms of reducing the peak in plasma concentration and maintenance of drug concentration in plasma, the chitosan granules were superior to conventional capsules.
Enantioselective Metabolism During Continuous Administration of S-(−)- and R-(+)-Nicotine Isomers to Guinea-Pigs
Authors: Nwosu C G , Godin C S , Houdi A A , Damani L A , Crooks P A 
Published: April 2011

Abstract
The S-(−)- and R-(+)-nicotine isomers were administered subcutaneously via Alzet osmotic pumps to male Hartley guinea-pigs (n = 5 with each isomer) over a 23-day period. Estimated dosage rate throughout the experiment was 0.6 mg−1. Urine samples were collected over this time and the levels of urinary oxidative and N-methylated nicotine metabolites were measured by cation-exchange HPLC analysis. S-(−)-Nicotine formed only oxidative metabolites, whereas the R-(+)-isomer formed both oxidative and N-methylated metabolites. 3′-Hydroxycotinine and nicotine-1′-oxide were major metabolites of both enantiomers; cotinine and nornicotine were only minor metabolites. The major N-methylated metabolite of R-(+)-nicotine was N-methylnicotinium ion; N-methylcotininium ion and N-methylnornicotinium ion were also identified as metabolites of this nicotine isomer. Total N-methylated quaternary ammonium metabolites accounted for 15 to 20% of the administered dose of R-(+)-nicotine. An interesting enantioselective reduction in the percent of oxidative urinary metabolites formed from S-(−)-nicotine was observed over 23 days. This may indicate the enantioselective induction of an uncharacterized metabolic pathway for this nicotine isomer.
Orally administered κ but not μ opiate agonists enhance gastric emptying of a solid canned food meal in dogs
Authors: Gué M , Fioramonti J , Junien J L , Bueno L 
Published: April 2011

Abstract
The effects of oral administration of selective mu (D-Ala2, N-Me-p-nitro-Phe4 Gly5-ol-DAGO, morphine) and/or kappa (3,4 dichloro-N-methyl N [2-(1. fyrrolidinyl) cyclohexyl]-benzene acetamide-U-50488, tifluadom) or mixed agonist (N-desmethyltrimebutine) opioid on gastric emptying have been evaluated using a radiolabeled [57Co] canned food meal in dogs fitted with gastric cannulas. In control conditions (placebo) the percentage of solids emptied 1 h after feeding was 27.3 ± 41%. When given orally at doses of 0.01 to 0.5 mg kg−1, U-50488 increased significantly (P &lt; 0.05) by 29.1 to 60.8% in a dose-related manner (r −0.94, P &lt; 0.01) the amount of gastric emptying of the meal in 1 h. This effect was reproduced by oral administration of tifluadom (0.01 to 0.1 mg kg−1)and by N-desmethyltrimebutine (0.1 to 1 mg kg−1). In contrast, the gastric emptying was unaffected by DAGO and morphine at low doses (0.01 and 0.1 mg kg−1) but significantly (P &lt; 0.05) slowed with higher doses of morphine. The increases in amount of gastric emptying induced by tifluadom, U-50488 and N-desmethyltrimebutine were abolished by previous administration of naloxone (0.1 mg kg−1 i.v.) and [(3-furylmethyl) noretazocine]-MR 22–66 (0.1 mg kg−1 i.v.). These results indicate that orally administered kappa, but not mu agonists at doses not exceeding 1 mg kg−1 enhance the amount of gastric emptying of a solid meal in dogs and suggest that this is due to a selective local stimulation of kappa mucosal or submucosal opiate receptors at antroduodenal level.
[3H]8-OH-DPAT labels the 5-Hydroxytryptamine uptake recognition site and the 5-HT1A binding site in the rat striatum
Authors: Alexander Beverley S , Wood Martyn D 
Published: April 2011

Abstract
The binding of [3H]8-hydroxy-2-(di-N-propylamino)-tetralin ([3H]8-OH-DPAT) to rat hippocampal and striatal membranes has been compared. In the hippocampus, low concentrations of [3H]8-OH-DPAT bound to a single, high affinity site which was sensitive to inhibition by spiperone, buspirone and ergotamine but not by mianserin, quipazine or (−)-propranolol. This is consistent with a selective labelling of the 5-HT1A receptor. In the striatum, [3H]8-OH-DPAT bound to two sites with high and low affinity (KD’s 1.18 and 109 nM). The high affinity component was blocked by low concentrations of buspirone, spiperone and ergotamine. The low affinity component was blocked only by high concentrations of buspirone and spiperone, and was not displaced by ergotamine at concentrations up to 1 μM. The ergotamine-resistant component of striatal [3H]8-OH-DPAT binding was blocked by low concentrations of the 5-HT uptake inhibitors fluvoxarmine and paroxetine, and by relatively low concentrations of 5-HT itself. Thus [3H]8-OH-DPAT labels the 5-HT transporter in the rat striatum. Unlike [3H]imipramine binding, the binding of [3H]8-OH-DPAT to the 5-HT transporter was independent of external sodium ions. It is therefore suggested that 8-OH-DPAT acts as substrate for the 5-HT transporter and labels the 5-HT recognition site of the transporter complex.
Effects of beclamide on isolation-induced aggression and locomotor activity in mice
Authors: Darmani N A , Sewell R D E , Nicholls P J 
Published: April 2011

Abstract
The anti-aggressive effects of orally administered beclamide (N-Benzyl-β-chloropropionamide) have been studied in male albino mice which were individually isolated for a 28-day period. Beclamide (50–250 mg kg−1 p.o.) caused an overall dose-dependent increase in the attack onset latency, a reduction in the percentage of animals attacking and the mean number of attacks/animal for this model of aggression. In addition, the highest dose of beclamide (250 mg kg−1 p.o.) did not significantly modify locomotor activity in mice. It was concluded that beclamide induced anti-aggressive effects at non-sedative doses. This anti-aggressive action was thought be at least partially mediated, through a beclamide-induced release of 5-HT from presynaptic sites.
Amelioration of the hypotensive effect of trypanocidal diamidines by use of heavy soluble salts
Authors: Steinmann U , Fritsch C 
Published: April 2011

Abstract
The influence of a heavy soluble dicaprylate salt preparation of a new trypanocidal diamidine (DiaPBF) on systolic and diastolic blood pressure and heart rate of rats has been compared with the effects of the easily soluble DiaPBF-dihydrochloride (DiaPBF-diHCl). After the dicaprylate the drop of the systolic blood pressure was 50% smaller than after an equimolar dosis of DiaPBF-diHCl.
Formulation Studies of Tableted Oral Rehydration Salt Mixtures
Authors: Ombaka Eva M A , Alkan M Hayat , Groves M J 
Published: April 2011

Abstract
Dehydration following non-specific diarrhoea may be prevented by oral administration of a simple glucose/salt mixture. A solution tablet of this mixture would have advantages of stability under environmental exposure and transport if the costs could be held within reasonable limits. The moisture adsorption and compression characteristics of Oral Rehydration Salts (ORS) ingredients have been studied. Combinations of ingredients resulted in a moisture adsorption higher than that of the individual components. This may be explained in terms of critical relative humidity, RHo, and environmental relative humidity RHi. Preparation of a stable ORS solution tablet therefore requires protection of moisture adsorbing components from the environment. The present UNICEF ORS mixture compacted easily by direct compression but gave fragile tablets, which were hygroscopic. This can be reduced by film coating the electrolyte component as granules with a resin (Eudragit L), or by simulating direct compression of the glucose as a compression-coating around the precompressed electrolytes. The packaging of compression-coated solution tablets in inexpensive polyethylene bags may lengthen the shelf-life and make the preparation less costly than the currently supplied ORS powders packed in laminated aluminium sachets. The increased dissolution lag time for the compacted tablet is a disadvantage that can be overcome by instructions to crush the product immediately before use.
Rectal Absorption of E-2078 (Dynorphin Analogue Peptide) in Rats
Authors: Murahashi Naokazu , Kato Akira , Koyama Noritoshi , Watanabe Sumio , Yuzuriha Teruaki , Miyake Yasuo 
Published: April 2011

Abstract
The plasma levels in rats of a dynorphin analogue peptide (E-2078) after rectal administration have been studied. The bioavailabilities of E-2078 after rectal administration, subcutaneous injection, intramuscular injection, and oral administration were 21·6, 67·8, 67·1, 0·7%, respectively. The effect of dose, pH, osmolarity and viscosity on the rectal absorption of E-2078 were studied. A sigmoid relationship between the dose and the AUC was observed on rectal administration, while there was a linear relationship on intramuscular administration. The AUC was increased in acidic solution and highly viscous solution. The osmolarity did not affect the absorption of E-2078. In microscopic studies, E-2078 caused little or no damage to the rectal mucosa in rats.
Biocompatibility of wound management products: the effect of various monosaccharides on L929 and 2002 fibroblast cells in culture
Authors: Schmidt Richard J , Spyratou Olga , Turner Terence D 
Published: April 2011

Abstract
The effects of various monosaccharides on the growth of human 2002 and mouse L929 fibroblast cultures have been investigated. Eleven monosaccharides having acidic, neutral, and basic characteristics were evaluated in a bioassay procedure developed for the investigation of biocompatibility of wound management materials. Rate of growth in both cell lines was inhibited by D-galacturonic acid and by D-glucuronic acid. Although most neutral sugars produced no significant change in the growth rate or in the morphology of the cells, galactose produced a significant increase in the growth rate of both cell lines whilst L-fucose caused a significant decrease in growth of the L929 cells but did not significantly affect the growth of 2002 cells; xylose increased the growth rate of L929 but not 2002 cells. D-Glucosamine, a basic sugar, produced inhibition of growth which followed a different pattern from that produced by the acidic sugars; N-acetylglucosamine produced a species specific increase in cell growth of L929 cells. The results show that the effects produced by the monosaccharides on the cultured fibroblasts are related to their chemical structure and to cell line, and suggest that the use of galactose as a possible aid to wound healing should be investigated.
Effectiveness of insulin suppositories in diabetic patients
Authors: Nishihata Toshiaki , Kamada Akira , Sakai Kiyoshi , Yagi Toshihito , Kawamori Ryuzo , Shichiri Motoaki 
Published: April 2011

Abstract
Experimental insulin suppositories regulated postprandial hyperglycaemia in diabetic patients. The insulin suppositories seemed also to avoid hyperinsulinaemia. The formulation with more rapid dissolution of insulin, which contained a solid dispersed form of insulin, effectively reduced the insulin dose required.
The Uptake and Translocation of Latex Nanospheres and Microspheres after Oral Administration to Rats
Authors: Jani P , Halbert G W , Langridge J , Florence A T 
Published: April 2011

Abstract
Non-ionic and carboxylated fluorescent polystyrene microspheres (100, 500 nm, 1 and 3 μm in diameter), were fed by gavage (2·5% w/v; 1·25 mg kg−1) daily for 10 days to female Sprague Dawley rats. Peyer’s patches, villi, liver, lymph nodes and spleen of animals fed the non-ionic microspheres from 100 nm to 1 μm showed unequivocal evidence of uptake and translocation of the particles. Heart, kidney and lung showed no evidence of the presence of microspheres. Carboxylated microspheres were taken up to a lesser degree than the non-ionised particles. Experiments with 125I radiolabeled 100 nm and 1 μm particles showed a higher uptake of the smaller particles, which were concentrated in GI tissue and liver. Particles were not distributed randomly in the tissues, but were concentrated at the serosal side of the Peyer’s patches and could be seen traversing the mesentery lymph vessels towards the lymph nodes. The results demonstrate a need to re-examine the possibilities of particulate oral delivery, as well as the potential toxicity of ingested particulates.
Ionization constants, octanol partition coefficients and Cholinesterase inhibitor constants for chlorpromazine and its metabolites
Authors: Whelpton Robin 
Published: April 2011

Abstract
The relationship between the lipophilic character of chlorpromazine and seven of its metabolites and their ability to inhibit horse serum Cholinesterase (Ki) has been investigated. Log(1/Ki) values were correlated with log P octanol partition coefficients (r = 0·88, P &lt; 0·01, n = 8). The inhibitor values ranged from 2·7 × 10−6 M for chlorpromazine to 48·6 × 10−6 M for monodesmethylchlorpromazine sulphoxide. Ionization constants were determined by limiting solubility, spectrophotometry and pH-partition characteristics. Demethylated metabolites were more basic than the tertiary amines and the sulphoxides were slightly less basic than the corresponding sulphides.