bluuebunny/crossref_metadata_2025_split huggingface dataset:
Biochemical and pharmacological tests for the prediction of ability of monoamine uptake blockers to inhibit the uptake of noradrenaline in-vivo: the effects of desipramine, maprotiline, femoxetine and citalopram
Authors: Pawłowski Leszek , Nowak Gabriel 
Published: April 2011

Abstract
The ability of desipramine and maprotiline (NA uptake inhibitors), as well as citalopram and femoxetine (5-HT uptake inhibitors) to protect mice against brain NA depletion induced by H 77/77 (4-α-dimethyl-m-tyramine), has been compared with their ability to counteract reserpine (2&#x006d;̇5 mg kg−1)- or apomorphine (16 mg kg−1)-induced hypothermia and to potentiate TRH (40 mg kg−1)-induced hyperthermia in mice. While both NA uptake inhibitors antagonized the action of H 77/77, maprotiline being weaker than desipramine, femoxetine and citalopram were inactive. However, in contrast to citalopram, femoxetine was active in the other tests, being about twice as weak as maprotiline, which itself was several times weaker than desipramine in those tests. On the basis of the results obtained it is concluded that functional in-vivo tests for NA uptake inhibitors are more sensitive than the H 77/77 biochemical test; moreover, femoxetine, which in in-vitro studies is less selective than citalopram, may inhibit the uptake of NA in-vivo.
Muscarinic receptor density is reduced in diabetic rat atria, an effect prevented by the aldose reductase inhibitor, Statil
Authors: Kofo-Abayomi A , Lucas P D 
Published: April 2011

Abstract
Binding assays using [3H]quinuclidinyl benzilate (QNB) as a muscarinic receptor ligand were carried out on atrial tissue from 6 control and 11 six-week streptozocin-diabetic rats. Five of the latter had received the aldose reductase inhibitor, Statil (25 mg kg−1 day−1 orally). Dissociation constants for specific (atropine displaceable QNB) binding were not changed either by diabetes or Statil treatment. Muscarinic receptor numbers, as estimated by Bmax values, were, however, significantly depressed in tissues from the untreated diabetic group, compared with tissues from either the controls or the Statil-treated diabetic group. These results may explain the reduced sensitivity to muscarinic agonists previously observed in atria from similarly diabetic rats and indicate the involvement of the sorbitol pathway in the change. Possible mechanisms are discussed.
Lymphoid tissue responses to a novel perfluorochemical emulsion in rats
Authors: Bollands A D , Lowe K C , Sharma S K , Davis S S 
Published: April 2011

Abstract
The effects of a novel perfluorochemical emulsion on rat lymphoid tissues and antibody production against sheep red blood cells (SRBC) have been studied. The responses were compared with those following injection of identical doses of the proprietary emulsion, Fluosol-DA 20% (F-DA). Liver weight was increased up to 15% at 8 days following intravenous (i.v.) or intraperitoneal (i.p.) injection of the novel emulsion but was unaffected by F-DA injection. Spleen weight also increased by a maximum of 20% in response to i.p. injection of the novel emulsion but this was less than increases of up to 44% which occurred in F-DA-injected rats. Thymus weight decreased (P &lt; 0&#x006d;̇05) following i.p. injection of the novel emulsion whereas mesenteric lymph node (MLN) weight remained unchanged. However, MLN weight was increased in response to i.v. injected F-DA, while thymus weight showed a small increase following i.p. F-DA injection. Mean plasma antibody titres to SRBC were significantly (P &lt; 0&#x006d;̇01) increased at 7 days after immunization in rats pretreated with i.p. injections of either the novel emulsion or F-DA; titres in animals pretreated with i.v. injections of either emulsion were similar to control.
Surface area and crystallinity of Form A of chloramphenicol palmitic and stearic esters: which one is the limiting factor in the enzymatic hydrolysis?
Authors: Forni F , Iannuccelli V , Cameroni R 
Published: April 2011

Abstract
Chloramphenicol stearic and palmitic esters in the polymorphic Form A, when ground for 85 h showed an in-vitro enzymatic hydrolysis rate constant (Khydr), the value of which was the same as that of a commercial Form B. The increase in the rate of the enzymatic hydrolysis was not related to the specific surface area as shown by the fact that the micronized Form A, having a higher specific surface area value than ground Form A, showed the same Khydr as the unground Form A. The Khydr value of the ground Form A could be the result of an increase in the crystalline disorder brought about by the grinding process.
An alteration in the liver microsomal membrane of the rat following paracetamol overdose
Authors: Araya Hiroshi , Horie Toshiharu , Hayashi Masahiro , Awazu Shoji 
Published: April 2011

Abstract
Fluorescence polarization of dansyl chloride covalently labelled microsomal membranes revealed an alteration in rat liver microsomal membranes following as a consequence of a paracetamol overdose. This suggests that dansyl chloride would be a useful probe in the study of the effects of paracetamol on microsomal membranes.
Comparative studies of cardiodepressant drugs on contraction dynamics and electrophysiological parameters of cardiac tissues at pH 7ṁ4 and 9
Authors: Schlieper P , Tawfik H 
Published: April 2011

Abstract
The effects of propranolol, amethocaine (tetracaine), lignocaine (lidocaine), procaine and benzocaine on force of contraction and action potential parameters of guinea-pig left atria and papillary muscles have been investigated at pH 7ṁ4 and 9. All the drugs decreased the force of contraction of both preparations. Their biological activities correlated with their lipid/buffer partition coefficients and with their ability to change the surface potential of liposomes. The sequence of activities is as follows: propranolol &gt; amethocaine &gt; lignocaine &gt; benzocaine &gt; procaine. Uncharged benzocaine had no effect on the liposome surface charge. Biological and physicochemical effects obtained at pH 9 were higher than those observed at pH 7ṁ4. Action potential amplitude and Vmax were decreased by all the drugs except benzocaine. At pH 9, the action potential duration was generally shortened, except by amethocaine and procaine; both caused a prolongation of the action potential at 90% repolarization.
Probenecid inhibition of the renal excretion of dyphylline in chicken, rat and man
Authors: Acara M , JR E A Carr , Terry E N 
Published: April 2011

Abstract
The effect of probenecid on the renal excretion of dyphylline was studied in chicken, rat and man. Dyphylline was found to be actively excreted when measured by the Sperber preparation in hens, the isolated perfused kidney of the rat and clearance studies in man. In each study probenecid significantly decreased dyphylline excretion demonstrating that dyphylline occupied the renal organic anion transport system. This same drug interaction, at the level of the renal excretory system, in these three species occurred at comparable concentrations of dyphylline and probenecid.
Enhanced penetration of mitomycin C through hairless mouse and rat skin by enhancers with terpene moieties
Authors: Okamoto Hirokazu , Ohyabu Makiko , Hashida Mitsuru , Sezaki Hitoshi 
Published: April 2011

Abstract
The effects of four new percutaneous absorption enhancers containing an azacyclo ring and terpene chain (l-geranylazacycloheptan-2-one (GAH), 1-farnesylazacycloheptan-2-one (FAH), 1-geranylazacyclopentan-2,***5-dione (GAPD), and 1-farnesylazacyclopentan-2-one (FAP)) and 1-dodecylazacycloheptan-2-one (Azone) on the percutaneous penetration of mitomycin C (MMC) through hairless mouse and rat skin in-vitro has been investigated. GAH, FAH, FAP and Azone enhanced MMC penetration by 20 to 60 times that of the control (ethanol). During the early part of the experiments, when the sink condition was maintained, FAH was the most effective for hairless mouse skin, whereas Azone showed the highest effect in the rat skin. The enhancing effect of GAPD was only about half that of the other enhancers, suggesting the importance of the polar group of the ring moiety in these compounds. The penetration of MMC through rat skin was also increased by pretreatment with these compounds, suggesting that the enhancers had a direct effect on the skin.
A high molecular weight form of pancreatic polypeptide was present in USP insulin and is absent in a more recent insulin preparation
Authors: Bauman William A , Meryn Siegfried 
Published: April 2011

Abstract
The concentrations and molecular forms of pancreatic polypeptide (PP) and glucagon were determined in USP XX and single-peak insulin preparations. In USP insulin the concentration of PP was 7 ng mg−1 insulin; on gel chromatography the PP immunoreactivity fractionated into two peaks of about equal size. One of the PP peaks was in the region of 4200 dalton PP, and the other PP peak eluted earlier in the region of a 7000-10***000 dalton peptide. The concentration of PP in single-peak insulin was 0ṁ8 ng mg−1 insulin; the immunoreactivity eluted in a single peak in the region of [125I]PP. The concentration of glucagon in each preparation was 55 ng mg−1 insulin. On gel chromatography the immunoreactive glucagon in each insulin preparation eluted in the region of [125I]glucagon.
The sorption of nitroglycerin by infusion sets
Authors: De Rudder D , Remon J P , Neyt E N 
Published: April 2011

Abstract
The sorption of nitroglycerin, from 5% glucose solution, by infusion sets was investigated under simulated perfusion conditions. Several burettes, sets and catheters were evaluated. The stability of the drug in the presence of glucose was also determined. High density polyethylene and glass proved satisfactory for its perfusion in solutions. A method for the evaluation of its uptake under simulated perfusion conditions is described.
Capsaicin-sensitive mechanisms and experimentally induced duodenal ulcers in rats
Authors: Maggi Carlo Alberto , Evangelista Stefano , Abelli Luigi , Somma Vincenzo , Meli Alberto 
Published: April 2011

Abstract
The incidence and degree of cysteamine- or dulcerozine-induced duodenal ulcers are increased by systemic capsaicin desensitization (50 mg kg−1 s.c. 4 days before) in adult rats. Acute administration of capsaicin, but not neurokinins or CGRP, produced a small but distinct plasma extravasation (Evans blue leakage) in the rat proximal duodenum which was absent in capsaicin-pretreated rats. These findings indicate the existence of a capsaicin-sensitive ‘duodenal defence mechanism’ in rats.
Inhibition of basal and insulin-stimulated gastric acid secretion by phenoxybenzamine or phentolamine
Authors: Salim Aws S 
Published: April 2011

Abstract
The present study in the rat was undertaken to investigate the possible involvement of α- and β-adrenoceptors in mediating gastric acid secretion in response to insulin-hypoglycaemia. Phenoxybenzamine, 15 mg kg−1, depressed the basal acid secretion to a level similar to that associated with vagotomy; phentolamine, 15 mg kg−1, had a similar effect. Insulin (1 unit kg−1) significantly stimulated gastric acid secretion. Vagotomy or phenoxybenzamine or phentolamine, 15 mg kg−1 prevented this action. The β-adrenoceptor blocking drug, propranolol, 5–15 mg kg−1, had no significant effect on the basal acid secretion or its stimulation by insulin. The similarity in action between vagotomy and large doses of phenoxybenzamine and phentolamine suggests that, in the rat, vagal α-adrenoceptor stimulation is involved in the mechanisms of basal and insulin-stimulated gastric acid secretion.
Anti-inflammatory activity of a polysaccharidic fraction of Echinacea angustifolia
Authors: Tubaro A , Tragni E , Del Negro P , Galli C L , Loggia R Della 
Published: April 2011

Abstract
The anti-inflammatory activity of a polysaccharidic fraction (EPF) obtained from Echinacea angustifolia roots has been examined using the carrageenan paw oedema and the croton oil ear test. EPF (0ṁ5 mg kg−1 i.v.) almost inhibited the carrageenan-induced oedema over 8 h and furthermore, EPF, topically applied, inhibited mouse ear oedema induced by croton oil. EPF also reduced the leukocytic infiltration of the croton oil dermatitis, evaluated both as peroxidase activity and histologically. After topical application EPF appears to be slightly inferior in potency to indomethacin. The results suggest that the anti-inflammatory activity of E. angustifolia resides in its polysaccharidic content.
The effect of molecular size on the nasal absorption of water-soluble compounds in the albino rat
Authors: Fisher A N , Brown K , Davis S S , Parr G D , Smith D A 
Published: April 2011

Abstract
The nasal absorption of a range of water-soluble compounds with different molecular weights, 4-oxo-4H-1-benzopyran-2-carboxylic acid (mol. wt 190), p-aminohippuric acid (mol. wt 194), inulin (mol. wt 5200) and dextran (mol. wt 70 000), has been investigated in the male Wistar rat. Compounds were instilled into the nasal cavities of anaesthetized animals and, for comparison, similar doses were administered intravenously. Serial samples of bile and urine were collected for up to 6 h. Nasal absorption, estimated by comparison of the extent of excretion in bile and urine following intranasal and intravenous administration, was 100% for 4-oxo-4H-1-benzopyran-2-carboxylic acid (1 mg kg−1), 75% for p-aminohippuric acid (1 mg kg−1), 15% for inulin (0&#x006d;̇1 mg kg−1) and 2&#x006d;̇8% for dextran (0&#x006d;̇25 mg kg−1). The log molecular weight gave a good linear correlation with the log per cent intranasally absorbed (correlation coefficient of -0&#x006d;̇996). From the molecular weight relationship, these data infer aqueous channel mechanisms for the nasal absorption of water-soluble compounds.
Evidence for tryptaminergic and noradrenergic involvement in the antisecretory action of morphine in the rat jejunum
Authors: Coupar Ian M , Taylor David A 
Published: April 2011

Abstract
Experiments have been performed to determine whether the antisecretory (antidiarrhoeal) effect of morphine in the intestine is mediated by a direct action of morphine on enteric nerves. Rats were pretreated with 6-hydroxydopamine (6-OHDA) or p-chlorophenylalanine (PCPA) to deplete intestinal stores of noradrenaline and 5-hydroxytryptamine (5-HT). Intraperitoneal injection of 6-OHDA (3 doses at 50 mg kg−1) caused a selective reduction in the level of noradrenaline in the jejunum to 7&#x006d;̇3% of control. Intraperitoneal injection of PCPA (200 mg kg−1) selectively reduced the jejunal level of 5-HT to 30&#x006d;̇5% of control. Groups of rats that had been treated as described above were anaesthetized and then injected intravenously with saline or with blocking doses of either atropine (0&#x006d;̇25 mg kg−1), hexamethonium (20 mg kg−1), ketanserin (30 μg kg−1), methysergide (30 μg kg−1), phentolamine (2 mg kg−1) or propranolol (1 mg kg−1). Following perfusion of the lumen of the jejunum, the rate of glucose absorption was measured to assess the integrity of the mucosa. Glucose absorption was unaltered in animals pretreated with hexamethonium and propranolol but there was a small enhancement in animals pretreated with atropine, PCPA, methysergide, 6-OHDA and phentolamine. The rate of net water absorption from the lumen of the jejunum and the rate of fluid secretion into the lumen following intra-arterial infusion of vasoactive intestinal peptide (VIP, 0&#x006d;̇8 μg min−1) were unaltered by any of the drug treatments. Intravenous injection of morphine (10 mg kg−1) did not alter the levels of noradrenaline or 5-HT in the whole jejunum. However, this dose of morphine did cause a 63&#x006d;̇5% decrease in the VIP-induced change in water transport. This antisecretory effect of morphine was unaltered in animals pretreated with atropine, hexamethonium and propranolol. In contrast, methysergide, ketanserin and 6-OHDA abolished the antisecretory effect of morphine. PCPA and phentolamine produced a partial inhibition of morphine's antisecretory effect. It is concluded that morphine produces its antisecretory effect in the jejunum by activation of noradrenergic and tryptaminergic systems.
The potentiation of phorbol ester-induced aggregation of human platelets by the prostaglandin endoperoxide analogue, U46619
Authors: Edwards Mary C , Williamson Elizabeth M , Evans Fred J 
Published: April 2011

Abstract
It was not possible to desensitize human blood platelets to 12-deoxyphorbol-phenylacetate (DOPP) stimulation in a manner analogous with that to platelet aggregating factor (PAF), prostaglandin-endoperoxide analogue (U46619) or adenosine diphosphate (ADP). Platelets previously desensitized to U46619, when challenged with DOPP and ADP, showed an increased aggregation and release of 5-HT. Sub-threshold aggregating doses of U46619 also caused a potentiation of the platelet response and release reaction to DOPP. The concentration of U46619 used to pretreat platelets affected the extent of potentiation of platelet stimulation induced by DOPP. The degree of potentiation was also affected by the time interval between addition of U46619 and DOPP. U46619 did not potentiate the aggregating effects of PAF, or ionophore A23187. The stimulus potentiation of DOPP by U46619 was abolished by prostacyclin (PGI2) and an antibody to U46619, but was unaffected by indomethacin and CP/CPK.
A new method for measuring the free fraction of cyclosporin in plasma by equilibrium dialysis
Authors: Henricsson S 
Published: April 2011

Abstract
The free fraction of cyclosporin in plasma has been measured by equilibrium dialysis in steel chambers. Equilibration time was 16 h. The intra-assay coefficient of variation was 7%. The free fraction remained constant in plasma samples frozen for up to 6 months, and was independent of the total concentration within the therapeutic range.
Activation of a myenteric 5-hydroxytryptamine-like receptor by metoclopramide
Authors: Sanger G J 
Published: April 2011

Abstract
Cholinergically mediated contractions were evoked by electrical field stimulation (EFS) of guinea-pig distal ileum longitudinal muscle-myenteric plexus strips. Metoclopramide, 0&#x006d;̇1–100 μM, dose-dependently increased the contractions, probably by increasing acetylcholine (ACh) release; contractions evoked by exogenous ACh in the presence of tetrodotoxin were not increased by metoclopramide. 5-Hydroxytryptamine (5-HT) 0&#x006d;̇3–30 nM similarly increased the height of the EFS-evoked contractions, although the maximum increase was less than for metoclopramide; higher concentrations of 5-HT (3 and 30 μM) had no effects or caused inhibition. The compound, ICS 205–930, 0&#x006d;̇001-1 μM, had no effect on the EFS-evoked contractions and caused inhibition at higher concentrations. Preincubation of the tissues with 5-HT, 0&#x006d;̇3–30 nM, did not affect the increase in EFS-evoked contractions caused by metoclopramide, 1 or 100 μM, whereas 5-HT, 3 and 30 μM, prevented the response caused by metoclopramide 1 μM, but not 100 μM. ICS 205–930, 0&#x006d;̇1 μM, had no effect on the increase in EFS-evoked contractions caused by metoclopramide 1 or 100 μM. The drug, at least in low concentrations, may therefore increase cholinergically mediated contractions of guinea-pig ileum by stimulating 5-HT-like receptors within the myenteric plexus, which differ from those antagonized by ICS 205–930.
Gossypol: a potent inhibitor of PAF-acether- and leukotriene-induced contractions of guinea-pig lung parenchyma strips
Authors: Touvay C , Vilain B , Sirois P , Soufir M , Braquet P 
Published: April 2011

Abstract
Gossypol, a substance extracted from cotton plants, markedly inhibited the contractile responses of guinea-pig lung parenchyma strips stimulated with leukotriene B4 (LTB4), leukotriene D4 (LTD4) and PAF-acether but not the responses to histamine (except at high concentration). It was slightly less potent than nordihydroguaiaretic acid (NDGA) and a PAF-antagonist (BN 52021). From previously reported effects of gossypol on the cyclooxygenase and lipoxygenases, and on the similarity of the inhibition produced by NDGA and gossypol on the lung parenchyma, it is suggested that the inhibition of the myotropic activity of the lung parenchyma by gossypol is due to interactions with the formation of cyclooxygenase products within the guinea-pig lung.
The oral clearance of zinc and triclosan after delivery from a dentifrice
Authors: Gilbert R J 
Published: April 2011

Abstract
Oral delivery and retention of zinc and triclosan were measured in man after use of an anti-plaque dentifrice containing these antibacterial agents. Triclosan (25% of the dose) and zinc (24%) were retained in the mouth immediately after toothbrushing and a single mouthrinse. Salivary concentrations fell from 7&#x006d;̇5 μg g−1 (triclosan) and 7&#x006d;̇0 μg g−1 (zinc) after 5 min to 0&#x006d;̇5 μg g−1 (triclosan) and 1&#x006d;̇2 μg g−1 (zinc), 2 h after brushing.
Autoregulation of renal blood flow during the infusion of acetylcholine or carbachol in anaesthetized dogs
Authors: Ogawa Nobuyaki , Ono Hiroshi 
Published: April 2011

Abstract
Whether renal blood flow autoregulation is abolished by acetylcholine was re-examined by kidney perfusion experiments in anaesthetized dogs. Renal blood flow was dose-dependently increased by the renal arterial infusion of acetylcholine (2 and 5 μg min−1) or another muscarinic agent, carbachol (2 and 5 μg min−1) and was maintained at an increased level during the infusion. When perfusion pressure was changed stepwise between 60 and 200 mmHg, the infusion of acetylcholine or carbachol caused no impairment of autoregulation. It is concluded that autoregulation is independent of muscarinic stimulation of vascular smooth muscle in the kidney.
Evaluation of sorghum starch as a tablet disintegrant and binder
Authors: Deshpande A V , Panya L B 
Published: April 2011

Abstract
The starch prepared from the seeds of Sorghum bicolor, Moench has been evaluated as a disintegrant and binder in tablets of magnesium sulphate, calcium carbonate, sulpha-dimidine, and chloroquine phosphate to represent soluble and insoluble inorganic and organic substances. The starch performed as well as maize starch in binding and disintegrating properties and better than acacia as binder.
Influence of pinacolyl dimethylphosphinate on soman storage in rats
Authors: Van Dongen C J , De Lange J 
Published: April 2011

Abstract
Atropinized rats pretreated with pinacolyl dimethylphosphinate (PDP) or saline were intoxicated with 6 x LD50 soman and, after 30 and 60 min, the absolute amounts of soman in diaphragms and lungs were measured gas chromatographically. The absolute amounts of free soman in both types of tissues were similar and were decreased after 60 min intoxication compared with the 30 min intoxication period. Pretreatment of rats with PDP reduced the amount of soman in the tissues by 63–78%. Incubation of isolated diaphragms and lungs with sodium fluoride (2&#x006d;̇5 mM) increased the amount of free soman in these tissues by 2&#x006d;̇6 X*** 103 and 16 times 103%, respectively. An assay to study the binding of tritiated PDP was developed. Although this assay was suitable to study the binding of tritiated quinuclidinyl benzilate to rat brain, no binding between tritiated PDP and diaphragm or brain tissue could be detected. It was concluded that PDP may counteract soman storage by another mechanism than occupation of binding sites.