bluuebunny/crossref_metadata_2025_split huggingface dataset:
Partial-solubility Parameters of Naproxen and Sodium Diclofenac
Authors: Bustamante Pilar , Peña Ma Angeles , Barra Jerome 
Published: April 2011

Abstract
The expanded Hansen method was tested for determination of the solubility parameters of two non-steroidal anti-inflammatory drugs, naproxen and sodium diclofenac. This work describes for the first time the application of the method to the sodium salt of a drug. The original dependent variable of the expanded Hansen method, involving the activity coefficient of the drug, was compared with the direct use of the logarithm of the mole fraction solubility lnX2 in the solubility models.
The solubility of both drugs was measured in pure solvents of several chemical classes and the activity coefficient was obtained from the molar heat and the temperature of fusion. Differential scanning calorimetry was performed on the original powder and on the solid phase after equilibration with the pure solvents, enabling detection of possible changes of the thermal properties of the solid phase that might change the value of the activity coefficient. The molar heat and temperature of fusion of sodium diclofenac could not be determined because this drug decomposed near the fusion temperature. The best results for both drugs were obtained with the dependent variable lnX2 in association with the four-parameter model which includes the acidic and basic partial-solubility parameters δa and δb instead of the Hansen hydrogen bonding parameter δh. Because the dispersion parameter does not vary greatly from one drug to another, the variation of solubility among solvents is largely a result of the dipolar and hydrogen-bonding parameters, a fact that is being consistently found for other drugs of small molecular weight.
These results support earlier findings with citric acid and paracetamol that the expanded Hansen approach is suitable for determining partial-solubility parameters. The modification introduced in the expanded Hansen method, i.e. the use of lnX2 as the dependent variable, provides better results than the activity coefficient used in the original method. This is advantageous for drugs such as sodium diclofenac for which the ideal solubility cannot be estimated. This paper shows for the first time that the method is suitable for determination of the partial-solubility parameters of a sodium salt of a drug, sodium diclofenac.
First-pass Metabolism of 5-Fluorouracil in Rats
Authors: Yuasa Hiroaki , Gu Jian , Hayashi Yayoi , Watanabe Jun 
Published: April 2011

Abstract
The first-pass metabolism of 5-fluorouracil has been investigated in rats to compare systemic bioavailability after administration by different routes, the bioavailability after intravenous bolus administration being defined as unity.
Bioavailability after oral administration (Fpo) was compared with that after intraintestinal administration into the closed loop (Floop) in conscious rats. Fpo was very low and variable (0.28 ± 0.30, mean ± s.d.), in agreement with earlier studies in man, but comparable with Floop (0.33 ± 0.05), suggesting insignificant loss of 5-fluorouracil by degradation in the gastrointestinal lumen or by faecal excretion. The bioavailability after intraportal vein administration (Fipv) was compared with Floop in rats anaesthetized with pentobarbital, anaesthesia being used to maintain a stable portal drug infusion that mimics the sustained input of drug into the portal blood flow after intra-intestinal administration. Fipv was smaller than unity (0.68 ± 0.03), suggesting significant hepatic first-pass metabolism, but higher than Floop (0.31 ± 0.10), suggesting significant first-pass metabolism in the intestinal mucosa. The intestinal bioavailability for passage through the epithelial mucosa (Fi) was estimated, from the ratio of Floop to Fipv, to be 046.
The study revealed that both the liver and intestinal mucosa are responsible for the extensive first-pass metabolism of 5-fluorouracil after oral administration. This first-pass metabolism might be similar to that in man, in which the oral bioavailability is reportedly similar to that in the rats used in this study. The findings in this study should be of help in monitoring ways of improving oral 5-fluorouracil therapy.
Different Contributions of the Endothelin ETA Receptor to Hypertension Induced by Acute or Chronic Inhibition of Nitric Oxide Synthesis
Authors: Hashimoto Norio , Kuro Toshihiko , Taira Shima , Matsumura Yasuo 
Published: April 2011

Abstract
The effects of FR139317(R)2-[(R)-2-[S)-2-[[1-(hexahydro-1H-azepinyl)]carbonyl] amino-4-methyl-pentanoyl] amino-3-[3-(1-methyl-1H-indoyl)]propionyl]-amino-3-(2-pyridyl)propionic acid), an endothelin ETA receptor antagonist, on systemic and renal haemodynamic responses and excretory responses to chronic or acute nitric oxide (NO) synthase inhibition with NG-nitro-L-arginine (NOARG) have been examined.
An intravenous bolus injection of FR139317 (10 mg kg−1) to chronic NO-deficient hypertensive rats (2.74 mM NOARG in drinking water for 4 weeks) elicited only a slight decrease in mean arterial pressure (MAP), to the same extent as seen in normotensive control rats. Injection of this drug induced no alteration of the renal haemodynamics of this chronic hypertensive model. Urine formation in control rats was significantly reduced by administration of FR139317. No significant decrease in urine formation was observed in the chronic NO-deficient rats. Acute intravenous injection of NOARG (5 mg kg−1) induced a gradual and significant increase in MAP, with a significant decrease in renal blood flow. A slight but insignificant diuretic effect was observed. In animals pretreated with FR139317 (10 mg kg−1 i.v.) NOARG induced a significantly less potent increase in MAP, whereas similar renal haemodynamic responses to NOARG were observed. In contrast to the FR139317-untreated group, urine formation tended to decrease after administration of NOARG. These results suggest that endothelin, via the ETA receptor, contributes to the systemic pressor response to acute NO synthase inhibition, although renal vasoconstriction and functional changes induced by acute NO synthase inhibition are independent of ETA receptor-related effects.
These results imply that action of endothelin via the ETA receptor is not involved in the maintenance of sustained hypertension induced by chronic NO synthase inhibition.
Inhibition of 15-Hydroxyprostaglandin Dehydrogenase Activity in Rabbit Gastric Antral Mucosa by Panaxynol Isolated from Oriental Medicines
Authors: Fujimoto Yohko , Sakuma Satoru , Komatsu Sawako , Sato Daisuke , Nishida Hiroko , Xiao Yong-Qing , Baba Kimiye , Fujita Tadashi 
Published: April 2011

Abstract
Panaxynol is a polyacetylene compound with anti-inflammatory and anti-platelet-aggregatory effects isolated from commonly used oriental medicines. The effects of panaxynol on the activity of prostaglandin-synthesizing and catabolizing enzymes in the rabbit gastric antral mucosa have been examined.
At concentrations ranging from 25 to 200 μM panaxynol had no effect on the synthesis of prostaglandins E2, F2α and D2 from exogenous arachidonic acid in the microsomal fraction of the gastric mucosa whereas at 25–200 μM it dose-dependently inhibited the activity of 15-hydroxyprostaglandin dehydrogenase (PGDH), which catalyses the initial step of prostaglandin catabolism, in the cytosolic fraction. The concentration required for 50% inhibition (IC50) was approximately 25 μM. Inhibition of PGDH by panaxynol was non-competitive with regard to NAD+ and prostaglandin E2.
These results suggest that panaxynol has the potential to inhibit PGDH activity in gastric mucosa, possibly as a result of pharmacological activity.
Pharmacological Properies of Pteleprenine, a Quinoline Alkaloid Extracted from Orixa japonica, on Guinea-pig Ileum and Canine Left Atrium
Authors: Seya Kazuhiko , Miki Izumi , Murata Kiyoshi , Junke Hisae , Motomura Shigeru , Araki Tsutomu , Itoyama Yasuto , Oshima Yoshiteru 
Published: April 2011

Abstract
We have investigated the pharmacological properties of pteleprenine, a quinoline alkaloid, on contractile responses of the guinea-pig ileum and on inotropic responses of the canine left atrium.
Although pteleprenine (0·1–1 μM) had no effect on the contraction of the ileum induced by acetylcholine at 10 μM it significantly inhibited acetylcholine-induced contraction of the ileum. Pteleprenine (0·1–10 μM) reduced nicotine induced-contraction of the ileum in a concentration-dependent manner yet had no maximum relaxant effect even at a concentration of 10 μM From Schild analysis the pA2 of pteleprenine on the guinea-pig ileum was found to be 6-6. The contraction of the ileum induced by 10 μM 1,1-dimethyl-4-phenylpiperazinium, a specific agonist of nicotinic acetylcholine. receptors, was concentration-dependently suppressed by 10 nM-10 μM pteleprenine. In contrast, 0.1–10 μM pteleprenine did not antagonize the acetylcholine- and nicotine-induced negative inotropic contractile responses of the canine left atrium. These results show that pteleprenine has inhibitory action against nicotinic acetylcholine receptors in the guinea-pig ileum but not in the canine left atrium. Our findings also suggest that pteleprenine might be a novel lead compound as a nicotinic receptor antagonist.
Behavioural Pharmacological Characteristics of Honokiol, an Anxiolytic Agent Present in Extracts of Magnolia Bark, Evaluated by an Elevated Plus-maze Test in Mice
Authors: Kuribara Hisashi , Stavinoha William B , Maruyama Yuji 
Published: April 2011

Abstract
Honokiol, a neolignane derivative of Magnolia bark, has central depressant action and, at much lower doses, anxiolytic activity. We have investigated the characteristics of the behavioural effects of honokiol by means of an elevated plus-maze test.
In the plus-maze test a single oral dose of 20 mg kg−1 honokiol significantly prolonged the time spent in the open arms of the maze, suggesting anxiolytic effect. Moreover, when honokiol was administered daily for seven days and the plus-maze test was conducted 3 or 24 h after the last administration, significant prolongation of the time in the open arms was manifested even for doses of 0.2 mg kg−1. The maximum effect was observed for doses of 0.5 mg kg−1. Honokiol at any dose in both single and repeated administration schedules caused neither change in motor activity nor disruption of traction performance. Orally administered diazepam, 0.5–2 mg kg−1, caused dose-dependent prolongation of the time spent in the open arms of the maze with a significant increase in motor activity at 1 mg kg−1, and dose-dependent disruption of traction performance. The changes in the plus-maze performance after treatment for seven days with 0.2 mg kg−1 honokiol and after a single treatment with 1 mg kg−1 diazepam were almost equivalent. The effect of honokiol (0.2 mg kg−1, treatment for seven days) was inhibited by subcutaneous flumazenil (0.3 mg kg−1) and (+)-bicuculline (0.1 mg kg−1) and by intraperitoneal CCK-4 (50 μg kg−1) and caffeine (30 mg kg−1). The anxiolytic effect of diazepam (1 mg kg−1) was also inhibited by flumazenil and bicuculline. However, the combined administration of diazepam with caffeine enhanced the effect, and diazepam completely reversed the effect of CCK-4.
These results suggest that, in contrast with diazepam, honokiol selectively induces an anxiolytic effect with less liability of eliciting motor dysfunction and sedation or dis-inhibition. The combined effects of the drug also revealed that the mechanism of anxiolytic effect of honokiol is partially different from that of diazepam.
DISPLAY‐CONTROL RELATIONSHIPS ON CIRCULAR AND LINEAR SCALES
Authors: LOVELESS N. E. 
Published: April 2011

variation in tracking performance between different quadrants of a circular scale has been shown to be attributable mainly to ambiguity of display‐control relationships on this scale, in that motion of pointer may be viewed as either rotary or translatory. dominant tendency is to view it as rotary, a clockwise control movement being associated with a clockwise pointer movement; but there is a significant secondary tendency to view it as translatory, a clockwise control movement being associated with a displacement of pointer upwards or to right, according to quadrant in which target lies. two tendencies conflict when target is in lower and right‐hand quadrants, where performance is consequently poorer. Performance is also affected by position in visual field as such.It has been verified that a clockwise control movement is expected to send pointer to right on a horizontal linear scale and upward on a vertical linear scale. Performance on horizontal scale is no better than that obtained on circular scale under optimal conditions, but unambiguity of linear scale renders it preferable where erroneous reactions are to be avoided.
PREVIOUS KNOWLEDGE AND MEMORY
Authors: POULTON E. C. 
Published: April 2011

This paper is concerned: (a) with the relationship between previous knowledge and memory, (b), with differences between recall and recognition, and (c) with set for time of memory test while learning. Subjects listened to 144 short statements, half of which were true and half false. They had to rate each statement on a five‐point scale for certainty of their truth or falsehood. A test of memory was then carried out for half of the statements, and another test was given a week later for the other half. In each test, half the statements had to be completed (recall), and each of the remaining statements had to be discriminated from a paired statement which resembled it in a standard way (recognition). While rating the statements, half the subjects did not expect a test of memory at all, a quarter were led to expect an immediate test, and the remaining quarter were led to expect a test in a week. After the first test of memory, no subjects were led to expect a second test. A control group of subjects took a test of ‘memory’ without hearing the statements.It was found that a subject was more likely to be certain that a false statement was false, than that a true statement was true. For both true and false statements, memory was best for statements about whose truth the subject was certain, and worst for statements about whose truth he had no idea. The control subject was much less successful than the experimental subject, but tended to score on the same statements. Previous knowledge can thus assist both genuine memory and also guess‐work.With memory for a particular word as a criterion, there was no difference between recall and two‐choice recognition when the word was in a statement about whose truth the subject was certain and correct, and memory was tested almost immediately. But recognition was more successful than recall when the word was in a statement about whose truth the subject had no idea, or when memory was tested after a week, although differences were only significant in the latter case.Recognition was found to be a less sensitive measure of previous knowledge than recall. Success in recognition was determined to a considerable extent by factors intrinsic to the test of recognition. Part of the reduced sensitivity of recognition was attributed to this cause.Immediate memory was best when a test of memory was expected immediately, and worst when no test was expected, but the differences were not significant. If anything, the trend for memory after a week was in the reverse direction.
FACTORS AFFECTING INDUCTIVE PREDICTIONS
Authors: GREEN R. T. 
Published: April 2011

Two guessing tasks which appear highly similar in nature nevertheless evoke opposite trends in predictive behaviour. Attempts to generate both sets of results from the same simple principles fail because of the different implicit assumptions the subject makes about the nature of the task. It would seem that one of the assumptions that the subject tends to make when required to employ inductive reasoning, at least in the laboratory situation, is that a certain amount of stimulus variability is to be expected.The theoretical implications are that, far from being contradictory or mutually exclusive, the gestalt and behaviourist accounts of the learning process are complementary. Only by recognizing that some aspects of the learning process are continuous while other aspects are discrete and that both S–R learning at an unverbalized level and conscious hypothesis testing go on side by side, is it possible to make sense of the more complex type of learning situation where a temporal pattern is involved.An attempt to analyse pre‐solution guessing behaviour tends to favour a non‐continuous hypothesis, but in certain respects the question is still open to a more sophisticated interpretation.
EYSENCK'S THEORIES OF ANXIETY AND HYSTERIA—A METHODOLOGICAL CRITIQUE
Authors: HAMILTON VERNON 
Published: April 2011

An examination is made of the evidence for and the validity of Eysenck's dimension of introversion‐extroversion. The dimension is found to be deficient on both counts, and therefore considered unsuitable as a starting‐point for further hypotheses. Eysenck's postulate and hypotheses linking introversion‐extraversion and anxiety and hysteria with cortical and reactive inhibition and with conditionability, satiation phenomena, reminiscence effects, etc., are discussed in relation to their predictive value and to the sufficiency of the evidence which has led Eysenck to conclude that his hypotheses have been confirmed.On the basis of a detailed review of Eysenck's findings, it is here concluded that the relationship between the continua of anxiety‐hysteria and of introversion‐extraversion has not been sufficiently demonstrated, and that the relationship between either of these continua and reactive inhibition and cortical inhibition represented by conditionability and satiation effects has not been established. It is further contended that there is insufficient empirical evidence for the identity of the inhibitory concepts used in the theoretical framework.
DEVELOPMENT OF THE PERCEPTION OF SOCIAL DIFFERENCES IN CHILDREN FROM 6 TO 10
Authors: JAHODA GUSTAV 
Published: April 2011

A specially devised pictorial technique to test the ability to perceive social differences, requiring a minimum of verbal instruction, was applied to a sample of 179 children systematically distributed according to age, sex and social status of parents. A performance test of intelligence and a vocabulary scale were also administered.An expected improvement with age was found with the social perception test, and there were significant sex and status differences. Analysis of covariance revealed that, except in the case of lower middle‐class girls, all status differences were in fact a consequence of the association between intelligence level and status, disappearing when the former was held constant.In discussing the children's responses it is shown that an incipient class concept can exist without the facility for giving it any verbal expression. An examination of the ways in which children build up a conceptual framework regarding social differences indicates that occupational divisions tend to come first with all children; later these are linked with differences in wealth, income and in the case of middle‐class children to some extent style of life. While a cognitive grasp of social differentiation is primarily dependent upon intellectual level, attitudes and feelings are largely determined by influences emanating from the child's particular social environment.
EXTRAVERSION‐INTROVERSION AND IMPROVEMENT IN AN AUDITORY VIGILANCE TASK*
Authors: BAKAN PAUL 
Published: April 2011

The study deals with the effect of a secondary signal‐detection task on performance in a primary signal‐detection task in an auditory vigilance situation. Forty subjects were tested under two conditions. In one condition they listened to an 80‐min. recording of a sequence of digits in order to detect the occurrence of primary signals defined as three successive odd digits which are all different. In another condition they listened for primary signals as described above, but in addition they also had to detect secondary signals defined as the occurrence of the digit68. The primary signals occurred ten times every 16 min.; there were about ten times as many secondary signals (digit 6) as there were primary signals (odd‐odd‐odd).The over‐all detection of primary signals was better when subjects were listening for both primary and secondary signals than when they listened for primary signals alone. Extraverts benefited more by the secondary task than introverts. No significant relationship was found between either neuroticism or intelligence and vigilance performance. A theoretical account of the events in a vigil is proposed and the difference between introverts and extraverts is considered in terms of this account.
ASSOCIATION BETWEEN MUSCULAR TENSION AND WORK OUTPUT*
Authors: FORREST D. W. 
Published: April 2011

E.M.G. electrodes were placed on the right forearm and chin of ten subjects while they performed simple addition. It was possible to record from one pair of electrodes the amount of muscular activity in the right forearm while the other pair indicated the moment of speaking and thus the speed of work.The variations in muscular tension and in speed of work were followed during the course of addition and this intra‐sum analysis revealed a different relationship from that found when larger units of work were taken. In the former case a marked tendency was found for increases in speed to be accompanied by low levels of tension, whereas when sums were taken as units no consistent relationship was apparent between the two variables within any one subject. This and other discrepancies are briefly discussed.
THE DYNAMIC STRUCTURE OF ATTITUDES IN ADULTS: A DESCRIPTION OF SOME ESTABLISHED FACTORS AND OF THEIR MEASUREMENT BY THE MOTIVATIONAL ANALYSIS TEST
Authors: CATTELL R. B. , HORN J. , BUTCHER H. J. 
Published: April 2011

In a systematic programme of research, two sets of factors have been repeatedly confirmed. Those of the first type are referred to as dynamic factors and comprise (a) drives or ‘ergs’ and (b) sentiments. These have been found when a wide range of adult attitudes has been measured by disguised tests and the results inter‐correlated and factor analysed. The factors of the second type are referred to as motivation components and are derived from the measurement of one attitude by many different devices.The number and nature of both types of factor are reviewed, and an experiment described in which a test battery was assembled so as to represent the principal factors of both types as economically and conveniently as possible. Thus for each expected dynamic factor two or more attitudes were included, all these attitudes being measured by four separate objective devices. The four objective devices were chosen to represent four of the most important components.From the results of this experiment, the Motivational Analysis Test was constructed, designed to measure, in a short testing time, ten drives and sentiments, each by four devices. The test battery is clinically and experimentally oriented, to cover such drives and sentiments as fear, narcissistic sex, parental sentiment and the self‐sentiment, for each of which a ‘conscious, integrated’ and an ‘unconscious, unintegrated’ score can be obtained, as well as a total score. Other established drives and sentiments with occupational and industrial relevance are included in another test battery still under construction.Some practical uses of the Motivational Analysis Test are briefly suggested.