bluuebunny/crossref_metadata_2025_split huggingface dataset:
Stimulant action of pethidine on the pregnant rat uterus in-vitro
Authors: Fazackerley J , Pleuvry B J 
Published: April 2011

Abstract
Pethidine's stimulant action on the 22-day pregnant rat isolated uterus does not involve receptors sensitive to methysergide and is unlikely to involve the synthesis and release of endogenous prostaglandins. The sensitivity of pethidine-induced contractions to verapamil suggests that mobilization of extracellular calcium is necessary for pethidine's action.
A comparative investigation of glycinebetaine and dimethylsulphoxide as liposome cryoprotectants
Authors: Higgins J , Hodges N A , Olliff C J , Phillips A J 
Published: April 2011

Abstract
The release of streptomycin from lecithin liposomes following a freeze-thaw cycle was used to measure the cryoprotective activities of glycinebetaine and dimethylsulphoxide (DMSO). At concentrations between 4 and 8% w/v in the external solution, glycinebetaine was superior to DMSO at freezing rates faster than 50 °C min−1. At lower rates their activities were similar, and drug loss ranged between 10 and 20% depending upon freezing rate and cryoprotectant concentration. The pattern of streptomycin loss when the concentrations of cryoprotectants inside and outside the liposome were varied indicated that glycinebetaine, in contrast to DMSO, does not diffuse across the liposome membrane. The activity of glycinebetaine was not impaired by the presence in the membrane of cholesterol or charged lipids.
The influence of viscosity on the migration of chloramphenicol and 4-hydroxybenzoic acid through glycerogelatin gels
Authors: Armstrong N Anthony , Gebre-Mariam Tsige , James Kenneth C , Kearney Patrick 
Published: April 2011

Abstract
Migration of chloramphenicol and 4-hydroxybenzoic acid from solutions in 1-octanol into Glycerol Suppository Base, BP and soft gelatin capsule shells is reported. Rates of migration through the gels, quantified in terms of diffusion coefficients, are given. An electron spin resonance probing technique was used to determine the microscopic viscosity. The latter, rather than the bulk viscosity, was shown to be the major rheological influence on the rate of diffusion.
Effect of moderate haemodilution with Fluosol-DA or normal saline on indocyanine green and (+)-propranolol kinetics
Authors: Shrewsbury Robert P , Lewis Lee M , Oliver Sharon R , Womble Catherine L 
Published: April 2011

Abstract
Indocyanine green (ICG) and (+)-propranolol kinetics were determined in the rat following moderate (50%) blood exchange with either Fluosol-DA or 0&#x006d;̇9% NaCl (saline). Rats received an intravenous ICG dose (5 mg kg−1) before an intravenous dose of (+)-propranolol (2&#x006d;̇5 mg kg−1) 0&#x006d;̇5, 24, 48 or 72 h after haemodilution and were compared with non-exchanged controls. Haemodilution with Fluosol-DA reduced the ICG elimination rate constant during the first 24 h while a significant reduction was seen 48 h after normal saline exchange. ICG clearances tended to be less than the control value, and were significantly reduced only at 24 h after Fluosol-DA exchange due to a reduced Varea. (+)-Propranolol half-life was significantly increased 48 and 72 h after saline exchange; (+)-propranolol clearance was only significantly reduced 72 h after Fluosol-DA exchange. ICG clearance may be reflecting a hypovolaemic change which occurs after haemodilution, which would reduce the hepatic blood flow. However, (+)-propranolol clearance was not altered, suggesting that the hepatic blood flow is not changed. It is possible that ICG clearance is changed due to alterations in its extraction ratio instead of hepatic blood flow changes.
Alcuronium pharmacodynamics in dogs: effect-concentration relationships in the diaphragmatic and limb muscles
Authors: Walker Judy S , Shanks Colin A , Borton Christopher , Brown Kenneth F 
Published: April 2011

Abstract
Previous studies suggest that the muscles of the diaphragm are less sensitive to neuromuscular blocking agents than the limb muscles. However, this difference has not been characterized directly in terms of relaxant drug plasma concentrations. The pharmacodynamics of the non-depolarizing muscle relaxant alcuronium were therefore investigated in nine dogs using a constant-rate infusion regimen with simultaneous measurement of muscle paralysis in the limb and diaphragm. Maximum paralysis between 95 and 100% was achieved in both muscle groups, within approximately the same time interval. However, during onset of and offset of effect, the pharmacodynamic parameters ECp50 and ECp95 for the limb muscle were lower than in the diaphragm. From a pharmacodynamic effect model it was also predicted that Css(50) and Css(95) for the limb muscles are half those values for the diaphragm. Thus, the diaphragm is less sensitive to the action of alcuronium than are limb muscles. The half-time for equilibration of alcuronium between plasma and the effect site was two-fold lower for the diaphragm, and the rate of recovery from paralysis in diaphragmatic muscles was twice that observed in limb muscles. Collectively, these data suggest that there is a greater margin of safety in the diaphragmatic muscles and that the response of the peripheral limb muscles to nerve stimulation provides only a conservative index of recovery from competitive neuromuscular block in the diaphragmatic muscles.
Fundamental properties of metronidazole formulations in relation to tableting
Authors: Itiola O A , Pilpel N 
Published: April 2011

Abstract
A study has been made of the effects of polyvinylpyrrolidone, gelatin and methylcellulose binding agents on the fundamental and tableting properties of a metronidazole-lactose-starch formulation. A material constant, α, was derived from the measured values of tensile strength of the materials. The values of a for the formulations are lower than that for metronidazole and depend on the nature and concentration of binder present. In terms of tableting properties, α supplements the information obtained from the ratios of elastic recovery to plastic compression (ER/PC) and from the brittle fracture index values (BFI) of the materials, although its influence appears to be limited at low values of ER/PC.
The presence of mucosa reduces the contractile response of the guinea-pig urinary bladder to substance P
Authors: Maggi Carlo Alberto , Santicioli Paolo , Parlani Massimo , Astolfi Mara , Patacchini Riccardo , Meli Alberto 
Published: April 2011

Abstract
The contractile response to substance P in-vitro is greater in strips of guinea-pig bladder freed of mucosa than in normal strips, while the response to field stimulation, histamine or KCl is unaffected by the presence of mucosa. Substance P has no inhibitory effect on histamine-induced contractions of the guinea-pig bladder. These findings support the possibility that the presence of mucosa may reduce accessibility of substance P to the muscle layer.
Liquid chromatographic determination of ampicillin and its metabolites in human urine by postcolumn alkaline degradation
Authors: Haginaka Jun , Wakai Junko 
Published: April 2011

Abstract
A high-performance liquid chromatographic method has been developed for the determination of ampicillin (I) and its metabolites ((5R, 6R)-penicilloate (II), the (5S, 6R)-epimer (III), and piperazine-2,5-dione (IV)) in human urine. The assay was based on the measurement of the absorbance at 300 nm following the postcolumn alkaline degradation with 0.75 M sodium hydroxide, 2 × 10−3 M mercuric chloride, and 1 × 10−2 M ethylenediaminetetraacetic acid disodium salt in solution. The limits of accurate determination were 0.5 μg mL−1 for I, 2.0 μg mL−1 for II and III, and 1.0 μg mL−1 for IV in neat urine samples with a 10 μL injection. At concentrations of compounds I-IV of 5 μg mL−1, within- and between-run precisions were 1.10–4.03% and 0.93–2.34%, respectively. The urinary levels of I and its metabolites were quantified by the proposed method.
Changes in glutathione and its metabolizing enzymes in human erythrocytes and lymphocytes with age
Authors: Al-Turk Walid A , Stohs Sidney J , El-Rashidy Fatma H , Othman Sadeq 
Published: April 2011

Abstract
The levels of glutathione (GSH) and the activities of glutathione S-transferases (GST) and glutathione reductase (GSR) in human erythrocytes and lymphocytes were determined in three age groups (5–12, 25–40, 65–83 years). The levels of GSH in lymphocytes increased with age, however, its levels in erythrocytes reached a maximum in the middle age group. The activity of GST in erythrocytes and lymphocytes changed as a function of age in a pattern similar to the changes found for GSH levels. GSR activity increased from young to middle age in both erythrocytes and lymphocytes, but decreased again in the old age group.
Solubilization kinetics of n-alkanes by a non-ionic surfactant
Authors: Donegan Ann C , Ward Anthony J I 
Published: April 2011

Abstract
The rates of solubilization of a homologous series of n-alkanes (CnH2n + 2; n = 8–16) into micellar solutions of n-dodecyl hexaoxyethylene glycol ether (C12E6) have been measured at 298 K. A mechanism involving a micellar dissociation-association process previously proposed was found to give an adequate description of the data. Proportionality between the micellar solubilization capacity in the kinetic process and that found at equilibrium could be inferred for such a series of solubilizates which have the same locus of solubilization and packing requirements.
Lipid vehicles for intestinal lymphatic drug absorption
Authors: Cheema M , Palin K J , Davis S S 
Published: April 2011

Abstract
The lipoprotein fractions in mesenteric lymph were monitored following intraduodenal administration of arachis oil and oleic, linoleic and linolenic fatty acids to rats. An increase in the chylomicron fraction, but not the VLDL or LDL fraction, was observed with each lipid. The greater the degree of unsaturation of the fatty acid, the more rapid the onset of chylomicron synthesis. The administration of linoleic acid and arachis oil produced the highest concentration of chylomicrons in the lymph. These results reflect differences in the rate of absorption and biochemical metabolism of the lipids and have implications for the selection of vehicles for the delivery of drugs by the lymphatic route.
Effects of dimethyl sulphoxide (DMSO) on aggregation of human blood platelets
Authors: Lehuu B , Curtis-Prior P B 
Published: April 2011

Abstract
The effects were examined of the universal solvent dimethyl sulphoxide (DMSO) on human platelet aggregatory activity, in-vitro, of the endogenous mediators ADP, adrenaline, arachidonic acid, collagen and PAF-acether which are believed to play important roles in cardiovascular diseases in man. DMSO inhibited aggregation induced by all of the mediators in the order ADP &gt; adrenaline = arachidonic acid = PAF-acether &gt; collagen. Since DMSO is widely used as a solvent for drug substances, an awareness of its intrinsic activity in any such evaluations is essential.
Involvement of Prostaglandin E-like Material in the Purgative Action of Rhein An throne, the Intraluminal Active Metabolite of Sennosides A and B in Mice
Authors: Yagi Teruyo , Miyawaki Yoshie , Nishikawa Tomoyo , Yamauchi Kazuko , Kuwano Shigeaki 
Published: April 2011

Abstract
Intracaecal administration of rhein anthrone, the intraluminally active metabolite of sennosides A and B, to mice quickly induced severe diarrhoea. Pretreatment with the prostaglandin (PG) biosynthesis inhibitor, indomethacin, and PGE2 antagonist, SC-19220, prevented the onset of diarrhoea induced by rhein anthrone, but the PGE2 antagonist polyphoretin phosphate (PPP) showed only a weak inhibitory effect. Rhein anthrone stimulated the production of PGE-like material only in the colon and its large intestinal propulsive activity was depressed by indomethacin and SC-19220, but not by PPP which suggests that the release of PGE-like material has some role in its purgative action.
Pharmacological Profile of New Histamine H2-Receptor Antagonists Related to Cimetidine, Ranitidine and Lamtidine
Authors: Orsetti M , Sorba G 
Published: April 2011

Abstract
New compounds structurally related to cimetidine, ranitidine and lamtidine have been prepared and tested for their histamine H2-receptor blocking activity on guinea-pig atria, rat perfused stomach and frog isolated gastric mucosa. These derivatives contain as a polar group, a diaminofurazan moiety, a 3-amino-4-methylfurazan or a 3-amino-4-phenylfurazan moiety. Ranitidine and lamtidine analogues display strong H2-antagonist activity in-vitro (KB on atria 0.037 μM and 0.0039 μM, respectively) and in-vivo on the lumen-perfused stomach of the anaesthetized rat (ID50 0.13 μmol kg−1 and 0.023 μmol kg−1 i.v., respectively). However, lamtidine analogues are ineffective in blocking the histamine-induced increase of H+ output in the frog isolated gastric mucosa. On the basis of the anomalous results in the frog, it is concluded that caution must be exercised in extrapolating information from amphibian to mammalian tissues with regard to the structure and the function of histamine receptors.
The inhibitory effect of liposome-encapsulated indomethacin on inflammation and platelet aggregation
Authors: Gürsoy Aylâ , Akbuğga JÜLi̇de , Eroğglu LÜTfi̇ye , Uluti̇n şengün 
Published: April 2011

Abstract
A comparison has been made between liposome-encapsulated and free indomethacin for their anti-inflammatory activities in the carrageenan paw oedema test in rats, and their inhibitory effect on platelet aggregation induced by adenosine 5-diphosphate (ADP) in-vitro. Free indomethacin, 3 mg kg−1, strongly inhibited carrageenan-induced oedema and a similar inhibitory activity was shown by 0.3 mg kg−1 of encapsulated drug. For the inhibition of platelet aggregation, the threshold concentration of free drug was 0.559 mM. At this concentration, at least 5 min incubation was needed to achieve 12.5% and 45 min for 50% inhibition. The inhibition was much stronger with encapsulated drug, and pre-incubation of 28 μM encapsulated drug for 10 min with platelet-rich plasma before addition of ADP completely inhibited platelet aggregation.
Myoclonic seizures in the mouse induced by alphaxalone and related steroid anaesthetics
Authors: File Sandra E , Simmonds Michael A 
Published: April 2011

Abstract
The anaesthetic steroids alphaxalone. 5β-alphaxalone and pregnanolone each caused myoclonic jerks in mice in a dose-related manner between 4 and 16 mg kg−1 i.v. There was no loss of righting reflex at these doses. The veterinary product Saffan, which contains alphaxalone and alphadalone, also caused myoclonic jerks at 2 mg kg−1 i.v., and a loss of righting reflex at doses of 4 mg kg−1 and above. These effects appear to be unrelated to the wide spectrum of potencies at the GABAA receptor complex of the three individual steroids as potentiators of muscimol, or as attenuators of picrotoxin.
Eudistomin derivatives, novel phosphodiesterase inhibitors: synthesis and relative activity
Authors: Kobayashi Jun'ichi , Taniguchi Mikio , Hino Tohru , Ohizumi Yasushi 
Published: April 2011

Abstract
The preparations of novel phosphodiesterase inhibitors, 8-acetoxy-5-iodo-6-methoxypy rido[3,4-b]indole, 5,7-dibromo-6-hydroxypyrido[3,4-b]indole, 5,7-dichloro-6-hydroxypyrido[3,4-b]-indole and 8-acetoxy-5-bromo-6-methoxypyrido[3,4-b]indole, are described together with concentrations giving 50% inhibition against cyclic AMP phosphodiesterase, i.e. 3 × 10−6, 3 × 10−6, 7 × 10−6 and 1 × 10−5 M, respectively. The relative potency of these eudistomin derivatives is discussed in terms of the chemical structures compared with those of other inactive eudistomins and derivatives.
Bunitrolol metabolism and its inhibition by cimetidine
Authors: Ishida Ryozo , Fujita Shoichi , Suzuki Tokuji 
Published: April 2011

Abstract
A simple fluorometric assay method as well as a sensitive HPLC method for determination of bunitrolol, a β-adrenoreceptor blocking drug, and its 4-hydroxylated metabolite is described. More than 90% of bunitrolol metabolized was accounted for by the formation of 4-hydroxybunitrolol in rat hepatic microsomes. Bunitrolol 4-hydroxylation required NADPH, and was inhibited by CO, proadifen and metyrapone, indicating that this reaction is mediated by cytochrome P450. This reaction was also inhibited by cimetidine competitively, and the inhibition constant, Ki, was 40 ± 11.5 μM (mean ± s.e. n = 3).
Effects of minaprine, a novel antidepressant, on prolactin secretion in the rat
Authors: Matsuo N , Yamada K , Kumacai M , Nagashima M , Matsumoto S , Shirakawa K , Furukawa T 
Published: April 2011

Abstract
The effect of minaprine, a novel psychotropic drug with antidepressant properties, on prolactin secretion has been investigated in the rat. On intraperitoneal administration (10 and 20 mg kg−1) it significantly decreased basal prolactin levels. In contrast, both haloperidol (1 mg kg−1 i.p.) and morphine (20 mg kg−1 i.p.) increased serum prolactin levels and daily treatment with oestradiol (100 μg kg−1 s.c.) for 4 days also elevated the levels. Minaprine at a dose of 20 mg kg−1 failed to antagonize the elevation of serum prolactin levels induced by these drugs. The results imply that minaprine may not exert a direct inhibitory action on prolactin secretion at the pituitary gland.
Effects of AN-132 and quinidine, antiarrhythmic agents, on plasma digoxin concentrations in rats
Authors: Sakai Kazushige , Yamazaki Tamotsu , Hinohara Yoshikazu 
Published: April 2011

Abstract
The effects of AN-132, 3-(diisopropylaminoethylamino)-2′,6′-dimethylpropionanilide.2H3PO4, on chloroform-induced arrhythmias and plasma digoxin concentrations have been compared with those of quinidine in rats. AN-132 (0.01–3 mg kg−1) administered orally significantly inhibited the incidence of cardiac arrhythmias in a dose-related fashion. A single dose of digoxin (1 mg kg−1) given orally for 7 consecutive days was followed, on day 8, orally by digoxin alone, or together with AN-132 (50, 100 and 200 mg kg−1) or quinidine (25 and 50 mg kg−1). The AUC0-24 and Cmax of plasma digoxin were enhanced significantly by co-administration of quinidine, but not by AN-132.
Influence of adrenocorticotrophic hormone on the behaviour in the swim test of rats treated chronically with desipramine
Authors: Volosin M , Cancela L , Molina V 
Published: April 2011

Abstract
Chronic desipramine (DMI) administration induced a dose-dependent reduction in the immobility time of the swim test in rats. A combined treatment of ACTH (50 iu kg−1 s.c.) and DMI (5 or 10 mg kg−1 i.p.) for 7 days potentiated the anti-immobility effect of DMI. ACTH 4–10, a fragment peptide with little corticotrophic activity, mimicked ACTH-induced potentiation. No stimulating effect on locomotor activity was observed following seven daily co-administrations of ACTH or ACTH 4–10 and DMI (10 mg kg−1). This behavioural evidence indicates that ACTH potentiation involves a central mechanism and demonstrates a functional interaction between ACTH and DMI at the behavioural level.
Compatibility of Intravenous Fat Emulsions with Prodrug Amino Acids
Authors: Ishii F , Takamura A , Ogata H 
Published: April 2011

Abstract
Three prodrugs, N-α-acetyl-L-arginine, N-α-acetyl-L-histidine and N-α-acetyl-L-lysine have been examined to see if they could induce significant changes in the stability of an intravenous fat emulsion, the stability being evaluated in terms of physicochemical measurements such as particle size distribution, surface tension, pH and zeta potential. The acetyl amino acids had an excellent stabilizing effect on the emulsion compared with amino acids without acetyl groups.
Differential Retention of Doxorubicin in the Organs of Two Strains of Rats
Authors: Chauffert Bruno , Dumas Monique , Dubuet Aleth , D'Athis Philippe , Olsson Nils Olivier 
Published: April 2011

Abstract
Fluorescence microscopy and high pressure liquid chromatography were used to study the decrease of doxorubicin (DXR) concentrations in the liver, spleen, heart, lung, kidney and skeletal muscle of two strains of rats at various times after a single intravenous injection of the drug (8 mg kg−1). DXR was located within the cell nucleus and was mostly undegraded, it persisted, especially in heart, lungs and spleen where it was detectable 10 days after injection. The DXR/DNA ratio, was used as an index of nuclear fixation of the drug. A major difference in the DXR/DNA ratio between the two strains were observed in heart and spleen results; the DXR/DNA ratio was significantly higher in heart and spleen compared with lung, liver and kidney in both strains.
Dose-dependency in the Exsorption of Theophylline and the Intestinal Dialysis of Theophylline by Oral Activated Charcoal in Rats
Authors: Arimori Kazuhiko , Nakano Masahiro 
Published: April 2011

Abstract
The elimination half-life of theophylline in serum after intravenous (i.v.) administration of aminophylline increased with increase in dose. Exsorption of theophylline from blood to the gastrointestinal tract was investigated after i.v. administration of aminophylline (10–50 mg kg−1) to rats by the in-situ single-pass perfusion technique. The exsorption rate of theophylline into the intestinal lumen also increased with increase in dose. When the dose of aminophylline was increased five-fold from 10 to 50 mg kg−1, the amount of theophylline exsorbed in 120 min was proportionally increased from 450 to 2300 μ g. The average extent of theophylline exsorbed into the intestinal lumen was 12–15% after doses from 10–50 mg kg−1, while the extent of the drug excreted into the bile varied from 0.17–0.30% after doses from 10–50 mg kg−1. However, intestinal and biliary clearance of theophylline did not change significantly in the range 10 to 50 mg kg−1. Oral administration of multiple doses of activated charcoal reduced the serum theophylline levels after i.v. administration of aminophylline (50 mg kg−1) to rats. The serum half-life and the area under the serum concentration-time curve of theophylline were decreased to 52 and 50% by the charcoal treatment, respectively, while the total body clearance of the drug was increased to 188% compared with the corresponding control experiments. The volume of distribution was not significantly different between treated and control rats. As the total body clearance after a high dose is less than after a low dose, because there is a decreased endogenous clearance (as observed in theophylline overdose), clearance after a high dose may be more enhanced by oral activated charcoal than that after a low dose.
Involvement of Prostaglandins in Histamine-induced Fluid and Electrolyte Secretion by Rat Colon
Authors: Hardcastle Jacqueline , Hardcastle P T 
Published: April 2011

Abstract
Histamine increased the transmural potential difference across rat colon in-vivo and induced a net secretion of fluid. Both effects were inhibited by indomethacin. Histamine increased the potential difference and short-circuit current, and reduced tissue resistance in colonic sheets in-vitro. This response was reduced in the absence of chloride in the bathing medium or in the presence of serosal frusemide, suggesting that histamine stimulated electrogenic chloride secretion by the colon. The rise in short-circuit current induced by histamine was calcium-dependent since it was reduced in the absence of serosal calcium or in the presence of serosal verapamil. Indomethacin, a cyclo-oxygenase inhibitor, and mepacrine, a phospholipase inhibitor, both caused a dose-dependent inhibition of the electrical response of colonic sheets to histamine, without affecting the rise in short-circuit current induced by prostaglandin E2. The stimulation of chloride secretion induced by histamine in rat colon therefore appears to be mediated by an increased production of prostaglandins.