bluuebunny/crossref_metadata_2025_split huggingface dataset:
Effects of Calcium Antagonists on the Erythrocyte Membrane
Authors: Abe Hiroko , Katada Keiko , Orita Machiko , Nishikibe Masaru 
Published: April 2011

Abstract
The effects of dihydropyridine compounds nimodipine, nicardipine and NB818 (isopropyl methyl-6-carbamoyloxymethyl-4-(2,3-dichlorophenyl)-1,4-dihydro-2-methyl-3,5-pyridine-dicarboxylate) on erythrocyte membranes have been studied. These compounds showed protective effects against hypotonic haemolysis, but not against heat-induced haemolysis. An increase in deformability of erythrocytes by these calcium antagonists was observed using a capillary tube centrifugal method. The erythrocytes showed slight stomatocytosis after 30 min of incubation with calcium antagonists, but did not show significant changes in mean corpuscular volume and ATP levels.
Two highly effective V1/V2 antagonists of vasopressin containing novel thioacids at position 1
Authors: Lammek B , Wang Y X , Franco R , Gavras I , Gavras H 
Published: April 2011

Abstract
In an attempt to develop more effective and selective V1/V2 antagonists of arginine vasopressin (AVP), two analogues have been designed and synthesized. In position 1 they contain thioacids that include a heteroatom in the cyclohexane ring. The 4-thio-4-tetrahydrothiopyraneacetic acid modification of position 1 used in one of them had advantages over the 1-mercaptocyclohexaneacetic acid substituted compound used as reference. The new compound was weaker at lower doses, but elicited a greater response at higher doses, whereas the reference compound reached its plateau earlier. Although the 4-thio-4-tetrahydropyraneacetic acid substitution used in the second compound resulted in a less potent analogue on a weight basis, this substitution also confers enhanced overall efficacy in terms of magnitude of effect.
Avoidance learning during antidepressant withdrawal in mice
Authors: Sansone Mario , Battaglia Mario , Ekblom Jonas , Nalepa Irena , Vetulani Jerzy 
Published: April 2011

Abstract
Shuttle-box avoidance acquisition, locomotor activity and density of adrenoreceptors in the cerebral cortex have been evaluated, in CD-I mice, during withdrawal from repeated treatment with desipramine or mianserin (5 or 14 daily injections of antidepressant drug, 10 mg kg−1). Withdrawal from mianserin did not produce any behavioural or neurochemical change. Mice withdrawn from desipramine exhibited avoidance facilitation, when training started 24 h (but not 72 or 120 h) after the last injection. Locomotor activity was not affected and no change was found in the density of β-adrenoreceptors. An up-regulation of α2- and, to a lesser extent, of α1-adrenoreceptors, occurred 72 h following desipramine withdrawal. However, the assessment of the role played by these neurochemical changes in the avoidance facilitation observed during withdrawal from the antidepressant treatment requires further study.
Inhibition of [3H]dopamine uptake by platelets by the dopamine-D2 receptor agonist RU 24926
Authors: Dean Brian , Srikanthan Preethi , Copolov David L 
Published: April 2011

Abstract
We have examined the effect of the dopamine-D2 receptor agonist RU 24926 (N-n-propyl-di-β(3-hydroxy-phenyl)-ethylamine HCl) on [3H]dopamine uptake by human platelets. RU 24926 reduced the uptake of [3H] dopamine by platelet-rich plasma and this affect was not reversed by the dopamine-D2 receptor antagonist haloperidol, or the dopamine-D1 receptor antagonist SCH 23390 (8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol). These data suggest that RU 24926 reduces [3H]dopamine uptake by platelets by competing for the dopamine uptake mechanism on the platelet and not by activation of the dopamine-D2 receptor.
Effect of 8-methoxypsoralen in the dark on proliferation of stimulated lymphocytes
Authors: Górski G , Antosz H , Gawron A 
Published: April 2011

Abstract
The effect of 8-methoxypsoralen (8-MOP) in the dark on proliferation of phytohaemagglutinin-stimulated human lymphocytes has been examined, using total blood leucocytes, the lymphocyte fraction and the T-lymphocyte subpopulation. 8-MOP (1 μg mL−1) increased [3H]TdR incorporation and caused a rise in the blastic and mitotic index in all experimental cultures. The lymphocyte proliferation in these experiments was effected by a comitogenic effect of 8-MOP on T-lymphocytes.
DNA strand breakage by peroxidase-activated mitoxantrone
Authors: Fisher Geoffrey R , Patterson Laurence H 
Published: April 2011

Abstract
Spectroscopic evidence demonstrates that the alkylaminoanthraquinone mitoxantrone is a substrate for horseradish peroxidase in the presence of hydrogen peroxide and that the result of this interaction is the formation of an air-stable mitoxantrone-derived free radical. The mitoxantrone-derived free radicals or their further oxidation products appear to extensively cross-link with plasmid DNA by a reaction that is mitoxantrone concentration-dependent. Oxidative activation of mitoxantrone to a DNA-damaging species may contribute to the mechanism of action of this antitumour agent.
In-vitro Dissolution Properties of Indomethacin Extended-release Capsules
Authors: Komuro Tetsuo , Yomota Chikako , Kimura Toshio 
Published: April 2011

Abstract
In-vitro dissolution properties of indomethacin extended-release capsules, from samples available on the Japanese market, have been investigated using a continuous flow, column-type dissolution apparatus and the results compared with those obtained by the paddle and the rotating basket methods. A plot of the percent of drug dissolved against the square root of time gave a straight line with the flow-through method but not with the paddle or the rotating basket methods. The results suggest an advantage of the flow-through method over the other two methods when extended-release products are tested by in-vitro dissolution.
Effect of an Anti-SRS-A Agent, NZ-107, on Airway Responses Induced by Ovalbumin and A23187 in the Guinea-pig
Authors: Yamamoto Akiko , Shikada Ken-Ichi , Iwama Takehisa , Sakashita Mitsuaki , Hibi Morihide , Tanaka Sakuya 
Published: April 2011

Abstract
The effects of the anti-SRS-A agent NZ-107 on antigen-(ovalbumin) and calcium ionophore A23187-induced airway responses in the guinea-pig have been investigated. In the presence of 5 μM indomethacin, NZ-107 (3 μM) did not affect the peak response in ovalbumin-induced contraction but did inhibit the prolonged response following the peak response in the tracheal strip. A higher concentration of NZ-107 (10 μM) completely blocked both peak and prolonged responses. Inhibitory effects of NZ-107 on ovalbumin responses were less in the lung parenchymal strip. The potency of NZ-107 in inhibiting ovalbumin-induced tracheal contraction was not changed in the absence of indomethacin but was reduced in the presence of 45 mM serine-borate, an inhibitor of the conversion of LTC4 to LTD4. NZ-107 inhibited A23187-induced contractions in both tracheal and parenchymal strips but in both cases the inhibitory potency was less than that on ovalbumin response. NZ-107 was a more potent inhibitor of ovalbumin-induced SRS-A release than histamine release in lung fragments but was ineffective in inhibiting A23187-induced SRS-A and histamine release. NZ-107 at a concentration of 10 μM more effectively inhibited LTC4-and histamine-induced tracheal contractions than it did LTC4 in the presence of 45 mM serine-borate. These results suggest that NZ-107 selectively inhibits antigen-induced SRS-A responses in airway tissues of the guinea-pig.
Investigations of the Possible Glycosylation of Monoamine Oxidase B from Pig Leucocytes
Authors: Balsa Maria Dolors , Gomez Néstor , Unzeta Mercedes 
Published: April 2011

Abstract
Monoamine oxidase B (MAO B) from pig liver has been reported to be a sialoglycoprotein. However, when that enzyme from pig lymphocytes and granulocytes was separated by polyacrylamide gel electrophoresis after labelling with the specific irreversible inhibitor [3H]pargyline, staining with 1-ethyl-2-[3-(1-ethyl-naphtho [1,2d] thiazolin-2-ylidene)-2-methylpropenyl] naphtho [1,2d] thiazolium bromide (“Stains-all”) failed to detect the presence of sialic acid residues. Treatment of the enzyme in disrupted lymphocytes and granulocytes, or in mitochondrial fractions prepared from them, with neuraminidase resulted in a decrease in MAO activity. However, after the enzyme was rendered soluble by treatment with octylglucoside, treatment with neuraminidase had no effect on the activity. These results indicate that sialic acid residues are not an intrinsic component of MAO B, although associated material containing such groups appears to affect the activity of the membrane-bound enzyme. The activities of membrane-bound preparations of MAO B from pig lymphocytes and granulocytes were unaffected by treatment with trypsin or β-chymotrypsin. After the preparations had been rendered soluble by treatment with octylglucoside there was a decrease in the activity on treatment with β-chymotrypsin, but trypsin treatment had no effect. Thus solubilization resulted in residues sensitive to cleavage by the former enzyme becoming accessible to it. Tryptic and chymotryptic peptides separated from the sodium dodecyl sulphate denatured enzymes by polyacrylamide gel electrophoresis revealed no differences between MAO B prepared from lymphocytes and granulocytes
The Extracellular Concentration of the Anti-epileptic Drug Valproate in the Rat Brain as Determined with Microdialysis and an Automated HPLC Procedure
Authors: Wolf J H , Van Der Duin L Veenma , Korf J 
Published: April 2011

Abstract
The cellular and extracellular brain concentration of valproic acid in freely moving rats has been estimated after intravenous injection of sodium valproate. Some rats were provided with a stereotaxically implanted dialysis probe in the striatum and a cannula in the heart through which the drug was injected and which allowed regular removal of blood. In other rats tissue levels of valproic acid were determined 5 and 90 min after drug injection. Valproic acid was determined by an automated precolumn derivatization procedure followed by HPLC separation and fluorimetric detection. Extracellular concentration was proportional to the blood concentration at every time interval, indicating rapid exchange of the drug between the two compartments. About 50% of the striatal content of valproate was in the extracellular space. The experiments demonstrated the usefulness of microdialysis to estimate both the extracellular concentration and the average cellular drug levels, provided a sensitive analysis procedure is available.
Extraction and Purification of Curcain, a Protease from the Latex of Jatropha curcas Linn
Authors: Nath L K , Dutta S K 
Published: April 2011

Abstract
A proteolytic enzyme, curcain, has been extracted from the latex of Jatropha curcas Linn. The enzyme was purified by chromatography on carboxymethyl cellulose and gel filtration on Sephadex G-200. The homogeneity of protein associated with curcain was established by non-denatured polyacrylamide gel electrophoresis using a discontinuous buffer system. The molecular weight of curcain was estimated by Sephadex G-100 gel filtration using a calibration curve of standard proteins to be around 22000 daltons.
External control of drug release and penetration: enhancement of the transdermal absorption of indomethacin by ultrasound irradiation
Authors: Miyazaki Shozo , Mizuoka Hideyuki , Oda Masako , Takada Masahiko 
Published: April 2011

Abstract
The effect of ultrasound (1 MHz) on transdermal absorption of indomethacin from an ointment has been studied in rats. Ultrasound energy was supplied for 10 min at a range of intensities (0.25, 0.5 and 0.75 W cm−2), energy levels commonly used for therapeutic purposes. The pronounced effect of ultrasound on transdermal absorption of indomethacin was observed for all three intensities studied. The mean AUC value (33.22 μg h mL−1) after irradiation at 0.75 W cm−2 was 3.4 times the control value (9.70 μg h mL−1).
The comparative bioavailability of cimetidine-alginate treatments
Authors: Britton A M , Nichols J D , Draper P R 
Published: April 2011

Abstract
The comparative bioavailability of cimetidine in cimetidine-alginate combinations has been investigated in twelve healthy volunteers in an open crossover study. Each volunteer received a single oral dose of a commercially available alginate-cimetidine combination tablet (Algitec) or cimetidine tablets (Tagamet), coadministered with a commercially available alginate reflux suppressant liquid or tablet (Gaviscon). No significant differences were observed between treatments for Cmax, tmax, AUC0–12 or AUC0-∞. The study demonstrated equivalent bioavailability of cimetidine when administered separately with alginate products and as a fixed dose combination product.
The influence of the γ-amino butyric acid (GABA) antagonist bicuculline on transport processes in rat small intestine
Authors: Hardcastle Jacqueline , Hardcastle P T , Mathias Wendy J 
Published: April 2011

Abstract
GABAergic involvement in the regulation of intestinal ion transport is suggested by the reduction in the short-circuit current generated by sheets of rat small intestine by the GABA antagonist bicuculline, although GABA itself caused no change. Bicuculline action was abolished by the inhibitor of Cl− secretion frusemide, suggesting that it involved a change in endogenous Cl− secretory tone. The effect of bicuculline appeared to be specific as it did not affect the electrical responses to glucose or exogenous secretagogues. The action of bicuculline was not observed in stripped intestinal sheets where the myenteric plexus is absent, and it was reduced by tetrodotoxin and atropine. It is suggested that endogenous GABA could be involved in the maintenance of a secretory tone in rat small intestine by acting on cholinergic mechanisms within the myenteric plexus.
α2-Adrenoceptor- and D2-dopamine receptor-mediated analgesic response of B-HT 920
Authors: Verma Anita , Kulkarni S K 
Published: April 2011

Abstract
The involvement of D2-dopamine receptors in the antinociceptive action of B-HT 920 (2-amino-6-allyl-5,6,7,8-tetrahydro-(4H) thiazolo-(4,5d)-azepine) has been investigated in mice. B-HT 920 (0.1–2.0 mg kg−1) and apomorphine (0.1–2.0 mg kg−1) produced a dose-dependent increase in tail flick latency. Analgesia induced by apomorphine was blocked by the D2-antagonist, haloperidol (1 mg kg−1) but not by the opioid antagonist, naloxone(1 mg kg−1). The antinociceptive action of B-HT 920 was potentiated by the D1-agonist SKF 38393 (5 mg kg−1), an action antagonized by haloperidol. The selective α2-adrenoceptor blocking drug yohimbine (1 mg kg−1) and naloxone (1 mg kg−1) blocked the antinociceptive action of B-HT 920 (1 mg kg−1). Haloperidol, however, failed to modify the B-HT 920-induced increase in tail flick latency. B-HT 920 and apomorphine reversed reserpine (2 mg kg−1) 4 h-induced hyperalgesia. The reversing action of apomorphine was blocked by haloperidol but not by yohimbine. Thus, a role of α2-adrenoceptors and D2-dopamine receptors is postulated in the antinociceptive action of B-HT 920.
Effect of nifedipine on Leishmania donovani infection in-vivo and in-vitro: chemiluminescence responses of peritoneal macrophages and neutrophils
Authors: Ganouly N K , Sodhi S , Kaul N , Kaur S , Malla N , Mahajan R C 
Published: April 2011

Abstract
After peritoneal macrophages had been exposed to different concentrations of nifedipine (10–120 ng mL−1) there was a significant increase (P &lt; 0.001) in the percentage of Leishmania donovani infected macrophages compared with controls. Parasite load was also significantly increased (P &lt; 0.001) in nifedipinetreated, L. donovani infected, BALB/c mice, compared with untreated, infected mice, post-inoculation. Peak chemiluminescence responses were significantly depressed (P &lt; 0.001) in nifedipinetreated infected mice compared with untreated mice post-inoculation. It is suggested that availability of intracellular calcium is a factor in the defense mechanism of inflammatory cells in L. donovani infections.
Plasma Protein Binding of Quinine: Binding to Human Serum Albumin, α1-Acid Glycoprotein and Plasma from Patients with Malaria
Authors: Wanwimolruk Sompon , Denton John R 
Published: April 2011

Abstract
The binding of quinine to human serum albumin (HSA), α1-acid glycoprotein (AAG) and plasma obtained from healthy subjects (10 Caucasians and 15 Thais) and from Thai patients with falciparum malaria (n = 20) has been investigated. In healthy volunteers, plasma protein binding expressed as the percentage of unbound quinine was 7·9–31·0% (69–92·1% bound). The mean percentage of unbound quinine found with essentially fatty acid-free HSA (40 g L−1) was 65·4±1 −5% (mean±s.d.) and was comparable with the value (66·3 ± 3·8%, mean ± s.d.) for Fraction V HSA (40 g L−1)- This suggests that fatty acids do not influence the plasma protein binding of quinine. Binding of quinine to 0·7 g L−1 AAG was high (mean unbound 61·0 ± 5·0%), indicating that quinine is bound primarily to AAG and albumin, although other plasma proteins such as lipoproteins may be involved. The mean percentage of unbound quinine was slightly less in Caucasians (14·8 ± 6·7% unbound), compared with healthy Thai subjects (17·0 ± 6·7% unbound). The higher binding of quinine in Caucasian subjects was associated with a higher plasma AAG concentration observed in Caucasians. Mean percentage of unbound quinine was significantly lower in Thai patients with malaria (10·9 ± 4·0%) than in the healthy Thai subjects. The increase in the extent of quinine binding corresponded with the increase in the acute-phase reactant protein, AAG in the patients with malaria. Overall, when the data were combined there was a significant correlation (r = 0·846, P &lt; 0·005) between the binding ratio (bound/unbound) of quinine and the plasma AAG concentration. This suggests that plasma AAG concentration may serve as a useful index to predict alterations in quinine binding. Although quinine is bound to albumin, it was not bound to either site I or site II on HSA as indicated from equilibrium dialysis and fluorescent probe displacement studies. Binding displacement studies revealed that there was no marked displacement of quinine by a variety of highly bound acidic and basic drugs, including other antimalarial drugs at their therapeutic concentrations.
Receptors Involved in the Modulation of 5-Hydroxytryptamine Release in Bovine Cerebral Arteries
Authors: Barrús Maria T , Marín Jesus , Villamor Jose , Balfagón Gloria 
Published: April 2011

Abstract
The uptake of [3H]5-hydroxytryptamine (5-HT) in bovine cerebral arteries was reduced by cocaine (1 μm), ouabain (100 μm), pretreatment with 6-hydroxydopamine (6-OHDA) (1·46 Mm, 10 min) and metitepine (1 μm). Electrically-stimulated tritium release was decreased by tetrodotoxin (0·8 μm), Ca-free medium, denervation with 6-OHDA (1·46 Mm, 10 min), 5-HT (10 μm), noradrenaline (1 μm) and the agonist of α2-adrenoceptors B-HT 920 (0·1 and 1 μm), enhanced by metitepine (1 μm, antagonists of presynaptic 5-HT1 receptors) and rauwolscine (1 μm, antagonist at α2-adrenoceptors, and also of 5-HT,1d receptors) and not affected by ketanserin (1 μm, antagonist of 5-HT2 receptors), methysergide (0·1 μm, antagonist of 5-HT1 and 5-HT2 receptors) and phentolamine (1 and 3 μm antagonist of α-adrenoceptors and less potent of 5-HT1 receptors). The inhibitory action of 10 μm 5-HT was partially reversed by phentolamine (3 μm) and cocaine (1 μm) and completely reversed by both metitepine (1 μm) and rauwolscine (1 μm). Ketanserin (1 μm), methysergide (0·1 μm) or phentolamine (1 μm) had no effect. Rauwolscine (1 μm) antagonized the inhibition induced by both noradrenaline (1 μm) and B-HT 920 (0·1 and 1 μm). 5-HT induced tritium release which was inhibited by cocaine (an antagonist of 5-HT3 receptors) and denervation with 6-OHDA. These results suggest that 5-HT is mainly accumulated in adrenergic nerve endings, that evoked [3H]5-HT release is modulated by 5-HT1-like receptors, but the participation of α2-adrenoceptors cannot be discounted, or more probably both types of receptors have features in common, and evoked [3H]5-HT release elicited by 5-HT may be partially mediated by activation of 5-HT3 receptors.
The Effect of Serum Ca2+ Compensation on the Efficacy of Chlorpropamide in Alloxan-diabetic Rabbits
Authors: Nishihata Toshiaki , Sakai Kiyoshi , Tsutsumi Ayumi , Fukui Miyuki , Yata Noboru 
Published: April 2011

Abstract
A decrease in serum Ca2+ concentration was observed in alloxan-diabetic rabbits, with recovery of serum Ca2+ levels achieved following insulin therapy. This suggested that the diabetic condition directly relates to the decrease in serum Ca2+ levels. The efficacy of chlorpropamide in alloxan-diabetic rabbits after intravenous injection (150 μmol kg−1) was less than that in normal rabbits as measured by the serum insulin levels, and the efficacy did not change when the dose was increased. However, compensation of serum Ca2+ levels in alloxan-diabetic rabbits caused an increase in the efficacy of chlorpropamide observed as an increase in serum insulin and a decrease in serum glucose levels.
Effect of mammalian lignans on f MLP-induced oxidative bursts in human polymorphonuclear leucocytes
Authors: Morikawa Masako , Fukuchi Kazunori , Inoue Michiko , Tsuboi Minoru 
Published: April 2011

Abstract
We examined the effects of mammalian lignans, enterolactone, prestegane B and 2,3-dibenzylbutane-1,4-diol (DBB) on superoxide production and luminol-dependent chemiluminescence (LCL) response in human polymorphonuclear leucocytes (PMNs). The three lignans had no direct effect on the responses of human PMNs. DBB and prestegane B enhanced the superoxide production and LCL response induced by formylmethionyl-leucyl-phenyl-alanine (f MLP), but enterolactone inhibited f MLP-induced effects. The effects of DBB were stronger than those of prestegane B and the effects of DBB were inhibited by bromophenacyl bromide, mepacrine, N-(6-aminophenyl)-5-chloro-t-naphthalene sulphonamide and trifluoroperazine, but not by gossypol, nordihydroguaretic acid, indomethacin, staurosporine, 1-(5-isoquinolinesulphonyl)-2-methylpiperazine dihydrochloride or (R,S)-2-methoxy-3-(octadecyl-car-bamoyloxy)-propyl-2-(2-thiazolio)-ethylphosphate. These results suggest that DBB primes the responses of human PMNs, and the priming effect is caused by the activation of phospholipase A2—and Ca2+ -calmodulin-pathways, but not by the activation of lipoxygenase, cyclo-oxygenase and protein kinase C or by the release of platelet activating factor.
Microsomal formation of N-benzyl-4-hydroxymethylaniline from N-benzyl-4-methylaniline
Authors: Ulgen M , Gorrod J W 
Published: April 2011

Abstract
The in-vitro metabolism of N-benzyl-4-methylaniline was re-examined using male hamster and rabbit hepatic microsomes; both species generated N-benzyl-4-hydroxymethylaniline, confirmed by TLC and HPLC, comparison with authentic compound. Further confirmation of the formation of this metabolite, was achieved by use of a rapid scan UV detector.