bluuebunny/crossref_metadata_2025 huggingface dataset:
Pharmacological Properties of Cannabinoid Receptors in the Avian Brain: Similarity of Rat and Chicken Cannabinoid1 Receptor Recognition Sites and Expression of Cannabinoid2 Receptor‐Like Immunoreactivity in the Embryonic Chick Brain
Authors: Fowler Christopher J. , Nilsson Olov , Andersson Mikael , Disney Graham , Jacobsson Stig O. P. , Tiger Gunnar
Published: August 2010

Abstract: The pharmacological properties of brain cannabinoid receptors were investigated in brains of 35 day‐old chickens, since little is known about the avian cannabinoid system. The cannabinoid1 receptor‐selective antagonist ligand [3H]SR 141716A bound to chicken brain membranes with KD and Bmax values of 0.92±0.28 nM and 790±58 fmol/mg protein, respectively. The binding was inhibited by CP 55,940 with a pI50 value of 7.63±0.14 and by a series of compounds with the order of potency CP 55,940>R(+)WIN 55,212–2>R‐1 methanandamide≈DAK. S(−)WIN 55,212–3 and AM404 were without inhibitory effect at 1 μM. Similar results were found for rat brain membranes. For both rat and chicken brain membranes, addition of the non‐hydrolysable GTP analogues Gpp[NH]p and GTPγS shifted the CP 55,940 inhibition curve to the right, consistent with an intact coupling to G‐proteins in the preparations. Fatty acid amidohydrolase in chicken brain membranes was less sensitive to inhibition by phenylmethylsulphonyl fluoride and arachidonoyl serotonin than its rodent equivalent. However, when fatty acid amidohydrolase activity in the preparations was reduced by use of a lower assay membrane concentration, anandamide was found to inhibit the binding of [3H]SR 141716A to chicken membranes with a pI50 value of 6.39±0.16. Using a novel antibody raised to amino acids 346–359 from the C‐terminal tail of the human cannabinoid2 receptor, it was found that embryonic chick brain tissue (and embryonic chick neurones in primary culture) expressed a ∼53 kDa immunoreactive band. This immunoreactivity, which was prevented by preincubation of the antibody with the immunising peptide, was also seen in cells expressing the recombinant human cannabinoid2 receptor, but was not seen in adult chicken brain homogenates or in rat cerebellar homogenates. However, a “classical” cannabinoid2‐receptor component of [3H]WIN 55212‐2 binding (i.e. a fraction inhibited by low concentrations of the cannabinoid2‐receptor‐selective antagonist SR 144528) was not found.
Protective Effect of Berberine on Cyclophosphamide‐Induced Haemorrhagic Cystitis in Rats
Authors: Xu Xinyun , Malavé Andrés
Published: August 2010

Abstract: The urotoxicity of cyclophosphamide and the protective effect of the herb berberine were investigated in this study. Administration of 150 mg/kg cyclophosphamide intraperitoneally caused a serious haemorrhagic cystitis in rats after 12 hr, including bladder oedema, haemorrhage, and dramatic elevation of nitric oxide metabolites (nitrite+nitrate) in urine and in plasma. To explore whether cyclophosphamide‐induced cystitis could be prevented by berberine, rats were pretreated with a single dose or two doses of berberine at 50, 100, or 200 mg/kg intraperitoneally then challenged with cyclophosphamide (150 mg/kg, intraperitoneally). The results indicated that pretreatment of rats with berberine could reduce cyclophosphamide‐induced cystitis in a dose‐dependent manner. Furthermore, we found that two doses of berberine showed greater protection against cyclophosphamide urotoxicity than when given a single dose. In addition, our data shows that a single dose of 200 mg/kg berberine, or two doses of 100, and 200 mg/kg berberine could completely block cyclophosphamide‐induced bladder oedema and haemorrhage, as well as nitric oxide metabolites increase in rat urine and plasma. In conclusion, our findings suggest that berberine could be a potential effective drug in the treatment of cyclophosphamide‐induced cystitis, and provides us with the bright hope in the prevention and treatment of cyclophosphamide urotoxicity.
Central Bromocriptine‐Induced Tachycardia is Reversed to Bradycardia in Conscious, Deoxycorticosterone Acetate‐Salt Hypertensive Rats
Authors: Lahlou Saad
Published: August 2010

Abstract: A central dopaminergic origin has been demonstrated for the bromocriptine‐induced tachycardia in conscious, normotensive rats. The present study investigated the effect of bromocriptine on heart rate and the principal site of action of this agonist in conscious, deoxycorticosterone acetate‐salt hypertensive rats, in which altered central dopaminergic activity has been previously reported. Intravenous administration of bromocriptine (150 μg/kg) increased heart rate (49±5 beats/min.) in uninephrectomized control rats, while it induced a significant bradycardia (50±6 beats/min.) in deoxycorticosterone acetate‐salt hypertensive rats. In the latter animals, intravenous (500 μg/kg) or intrathecal (40 μg/rat at T9–T10) pretreatment with domperidone, a selective dopamine D2 receptor antagonist that does not cross the blood‐brain barrier, reduced partially, but significantly, the bradycardiac responses to bromocriptine (reduction of about 44% and 48% of the maximal effect, respectively). In contrast, the bromocriptine‐induced bradycardia was fully abolished by intravenous pretreatment with metoclopramide (300 μg/kg), a dopamine D2 receptor antagonist that crosses the blood‐brain barrier, or by combined pretreatment with intravenous and intrathecal domperidone. These results indicate that, in deoxycorticosterone acetate‐salt hypertensive rats, bromocriptine decreases rather than increases heart rate, an effect that is mediated partly through a peripheral D2 dopaminergic mechanism and partly through stimulation of spinal dopamine D2 receptors. They further support the concept that, in normotensive, conscious rats, the central tachycardia of bromocriptine appears to predominate and to mask the bradycardia of this agonist at both peripheral and spinal dopamine D2 receptors.
Role of Metabolism in Arsenic Toxicity
Authors: Vahter Marie , Concha Gabriela
Published: August 2010

Abstract: In humans, as in most mammalian species, inorganic arsenic is methylated to methylarsonic acid (MMA) and dimethylarsinic acid (DMA) by alternating reduction of pentavalent arsenic to trivalent and addition of a methyl group from S‐adenosylmethionine. The methylation of inorganic arsenic may be considered a detoxification mechanism, as the end metabolites, MMA and DMA, are less reactive with tissue constituents, less toxic, and more readily excreted in the urine than is inorganic arsenic, especially the trivalent form (AsIII, arsenite). The latter is highly reactive with tissue components, due to its strong affinity for sulfhydryl groups. Thus, following exposure to AsV, the first step in the biotransformation, i.e. the reduction to AsIII, may be considered a bioactivation. Also, reactive intermediate metabolites of high toxicity, mainly MMAIII, may be formed and distributed to tissues. Low levels of MMAIII, DMAIII have been detected in urine of individuals chronically exposed to inorganic arsenic via drinking water. However, the contribution of MMAIII, DMAIII to the toxicity observed after intake of inorganic arsenic by humans remains to be elucidated. The major route of excretion of arsenic is via the kidneys. Evaluation of the methylation of arsenic is mainly based on the relative amounts of the different metabolites in urine. On average human urine contains 10–30% inorganic arsenic, 10–20% MMA and 60–80% DMA.
Effect of Tiagabine and Topiramate on Porphyrin Metabolism in an in vivo Model of Porphyria
Authors: Krijt Jan , Krijtová Hana , Sanitrák Jaroslav
Published: August 2010

Abstract: Administration of many antiepileptic drugs to patients with porphyria can precipitate an acute porphyric crisis. Information on the porphyrogenic activity of new antiepileptic drugs is still limited. In the presented study, the effects of tiagabine and topiramate on porphyrin metabolism were evaluated in an in vivo model of porphyria. Administration of the protoporphyrinogen oxidase inhibitor oxadiazon (12.5 mg/kg/day) for four days to male Wistar rats caused a partial block of porphyrin biosynthesis, thus mimicking the condition of quiescent variegate porphyria. Administration of phenobarbital (75 mg/kg/day) to oxadiazon‐pretreated rats increased liver porphyrin content, liver porphobilinogen content (means 480 nmol/g, control less than 20 nmol/g) and urinary excretion of porphobilinogen (means 1000 μmol/l, control less than 20 μmol/l). Tiagabine (75 mg/kg/day) and topiramate (75 mg/kg/day) increased liver porphobilinogen content (means 33 and 53 nmol/g respectively) and urinary porphobilinogen concentration (240 and 490 μmol/l respectively). Similar results were obtained in oxadiazon‐treated BALB/c mice. In untreated rats, tiagabine and topiramate caused a moderate increase of hepatic pentoxyresorufin‐O‐dealkylase activity (approximately 100 and 200 pmol/min./mg respectively, controls 15 pmol/min./mg). These data demonstrate that administration of tiagabine or topiramate to oxadiazon‐treated animals can provoke a condition resembling an acute porphyric attack and suggest that administration of these drugs to patients with suspected porphyria should be avoided. However, 5‐day administration of both tiagabine and topiramate (75 mg/kg) is considerably less porphyrogenic than phenobarbital administered at the same dose.
Generation of Hydroxyl Radicals by the Antiviral Compound Phosphonoformic Acid (Foscarnet)
Authors: Lindqvist Christer , Nordström Tommy
Published: August 2010

Abstract: Phosphonoformic acid (foscarnet) is an antiviral agent that is used to treat severe cytomegalovirus infections in AIDS patients. We demonstrate by using the ferrous iron indicator Ferrozine and ascorbic acid (vitamin C) that foscarnet can chelate ferric iron and form a redox‐active iron complex. By using the hydroxyl radical indicator coumarin‐3‐carboxylic acid we found that the foscarnet‐Fe3 complex formed can readily catalyze hydroxyl radical (˙OH) generation by the Fenton reaction: (Fe2++ H2O2→Fe3++˙OH +−OH) if hydrogen peroxide and ascorbic acid are present. Hydroxylation of coumarin‐3‐carboxylic acid could be blocked by addition of known hydroxyl radical scavengers such as mannitol, sucrose, glucose and dimethyl sulfoxide. Moreover, by using a DNA nicking assay, we found that foscarnet catalyzed hydroxyl radicals can induce single strand brakes in DNA. The potency of the hydroxyl radicals formed to induce damage could also be demonstrated in a phosphate‐free buffer where the hydroxyl radicals formed attacked and liberated phosphate from the foscarnet molecule. Our results indicate that foscarnet catalyzed hydroxyl radical formation might take place during conditions where a peroxide generating system(s), vitamin C and transitions metals are present.
Ocular Changes after Intravitreal Injection of Methanol, Formaldehyde, or Formate in Rabbits
Authors: Hayasaka Yoriko , Hayasaka Seiji , Nagaki Yasunori
Published: August 2010

Abstract: We evaluated the effects of intravitreal injection of methanol, formaldehyde, or formate on rabbit eyes. One hundred μl of 1% methanol, 1% or 0.1% formaldehyde, or 1% formate was injected in the vitreous cavity of the right eyes of rabbits. The eyes were examined by biomicroscopy and ophthalmoscopy weekly. One month after injection, the eyes were enucleated and examined histologically. One week after treatment the animals that received 0.1% formaldehyde showed retinal vessel dilation, and the rabbits that received 1% formaldehyde showed mild posterior subcapsular cataract and retinal vessel dilation and haemorrhages. One month after treatment, the animals that received 0.1% or 1% formaldehyde developed mild posterior subcapsular cataract and retinal lesions. Animals that received 1% methanol or 1% formate showed nearly normal optical media and fundi. Histologically disorganized retina and optic nerve were seen in eyes that received 0.1% or 1% formaldehyde. Eyes that received 1% methanol or 1% formate appeared histologically normal. Our findings indicate that intravitreal injection of formaldehyde causes retinal and optic nerve damage, while methanol and formate are not or less toxic to ocular tissues.
Gene Induction by Phenobarbital: An Update on an Old Question that Receives Key Novel Answers
Authors: Corcos Laurent , Lagadic‐Gossmann Dominique
Published: August 2010

Abstract: Phenobarbital has long been used as a sedative and antiepileptic drug. The drug is the representative of a myriad of lipophilic molecules able to evoke a pleiotropic response in the liver and also in prokaryotes and flies. A great deal of novel information has been obtained in recent years regarding the mechanism of cytochrome P450 (CYP) gene induction by phenobarbital. Most importantly, a nuclear orphan receptor, the constitutive androstane receptor has been identified as a primary determinant of the transcriptional activation of CYP genes in response to phenobarbital‐like inducers in mammals. Another nuclear receptor, the pregnane X receptor can also mediate some of the phenobarbital response, but the functional overlap of the two inductive pathways is only partial. The response of mammalian CYP2B genes to phenobarbital was abolished in the liver of mice carrying a null allele of the constitutive androstane receptor gene, whereas that of CYP3A genes was lost in pregnane X receptor knock‐out mice.
Electrophysiological and Neurochemical Evidence for Voltage‐Dependent Ca2+ Channel Blockade by a Novel Neuroprotective Agent NS‐7
Authors: Oka Michiko , Hayashi Seiji , Itoh Yoshinori
Published: August 2010

Abstract: The effects of a neuroprotective agent 4‐(4‐fluorophenyl)‐2‐methyl‐6‐(5‐piperidinopentyloxy) pyrimidine hydrochloride (NS‐7) on the Ca2+ currents in rat dorsal root ganglion neurones and on the depolarization‐evoked nitric oxide synthesis, which was estimated from cyclic GMP formation in slices of the rat cerebral cortex, were investigated, and its mode of action was compared with those of typical Ca2+ channel blockers. In rat dorsal root ganglion neurones, NS‐7 (0.3–100 μM) inhibited the whole‐cell Ba2+ currents (IBa) in a voltage‐dependent manner, in which the compound more potently blocked the IBa elicited from the holding potential of −40 mV than that induced from −80 mV. In slices of rat cerebral cortex, KCl‐evoked nitric oxide synthesis was markedly inhibited by ω‐conotoxin GVIA and ω‐agatoxin IVA, but only slightly attenuated by nifedipine, suggesting that the response is mediated predominantly through activation of N‐type and P/Q‐type Ca2+ channels. NS‐7 (1–100 μM) inhibited the KCl‐stimulated nitric oxide synthesis in a manner dependent on the intensity of the depolarizing stimuli. Moreover, weak but significant inhibitory effect of NS‐7 was observed even after wash‐out. Similar voltage‐dependent inhibition of the KCl response was observed by a limited concentration (10 μM) of verapamil. These findings indicate that NS‐7 in several concentrations blocks Ca2+ channel in a voltage‐dependent manner.
Bisphosphonates and Nephrocalcinosis in a Rabbit Leg Lengthening Model: A Histological and Therapeutic Comparison
Authors: Williams Paul R. , Smith Nicholas C. , Cooke‐Yarborough Claire , Little David G.
Published: August 2010

Abstract: We performed a comparison of the effects of two bisphosphonates, pamidronate and zoledronic acid, on regenerate bone mineral content in distraction osteogenesis in an immature rabbit model. Single dose zoledronic acid was found to be 18 times more potent at producing an increase in bone mineral content than pamidronate per mg/kg of drug infused at surgery. Histological examination of all rabbit kidneys was performed at trial completion. Nephrocalcinosis was identified in 14 of 20 kidneys of rabbits infused with pamidronate, but was not detected in the 20 kidneys of those rabbits infused with zoledronic acid. A further 20 kidneys from rabbits given a second dose of zoledronic acid were also found to be free of signs of nephrocalcinosis. Three of 40 control kidneys exhibited signs of nephrocalcinosis. The increased potency of zoledronic acid allowed us to give one‐tenth the dose of pamidronate, with increased therapeutic efficacy and no evidence of nephrocalcinosis.
A New Method to Evaluate in vitro Myelotoxicity of Antitumour Agents in the First Steps of Drug Development
Authors: Ferlini Cristiano , Distefano Mariagrazia , Pierelli Luca , Bonanno Giuseppina , Fattorossi Andrea , Battaglia Alessandra , Mancuso Salvatore , Scambia Giovanni
Published: August 2010

Abstract: Research focused on the development of new anticancer agents has been based mainly on the assessment of the antitumour activity. This yields a large number of newly developed drugs endowed with good antitumour properties, but heavy side‐effects on myelopoiesis. In this work, we validate a new method potentially useful to assess myelotoxic effect of newly developed agents. The proposed technique uses peripheral blood CD34+ cells as source of haematopoietic progenitors. These cells are grown in liquid culture in the presence of cytokines able to induce differentiation versus the three main lineages. Doxorubicin, carboplatin and topotecan served as reference drugs to investigate the accuracy of the technique. The three drugs mimick the effects reported in vivo. Doxorubicin and carboplatin produce a specific effect toward erythropoietic and thrombopoietic lineages, respectively, and topotecan a three‐lineage toxicity. An advantage of the technique is the possibility to further investigate myelotoxicity. Here, we assessed differentiation markers in CD34+ cells to evaluate if the three drug treatments can affect the process of differentiation. Data show that the drug treatments were unable to modulate the expression of the selected differentiation markers in the surviving population. We propose this method as an innovative tool to score the myelotoxic effect of compounds in the first steps of drug development to further develop those compounds with the best ratio between activity and myelotoxic effects. Moreover, the fact that the method is performed in liquid phase allows its optimisation in a conventional “high throughput system”.
Role of Monoamine Oxidase Inhibition and Monoamine Depletion in Fenfluramine‐Induced Neurotoxicity and Serotonin Release
Authors: Halladay Alycia K. , Kirschner Emily , Hesse Kelly , Fisher Hans , Wagner George C.
Published: August 2010

Abstract: The role of both monoamine synthesis and monoamine oxidase inhibition in mediating the fenfluramine‐induced damage to serotonin neurones was examined; as pretreatment agents, both alpha‐methyl‐para‐tyrosine (AMPT) and para‐chlorophenylalanine (PCPA) were used to deplete dopamine and serotonin, respectively, while clorgyline and deprenyl were used to inhibit monoamine oxidase types A and B. While both AMPT and deprenyl did not alter fenfluramine‐induced serotonin or 5‐hydroxyindoleacetic acid (5‐HIAA) depletion in any area, PCPA did partially reduce the serotonin depletion in the hippocampus and hypothalamus. Although pretreatment with clorgyline did not significantly alter fenfluramine‐induced serotonin depletion, it did produce a 65% mortality rate in animals treated with both drugs. Both PCPA and clorgyline significantly increased the depletion of striatal 5‐HIAA concentration consequent to fenfluramine; however, these drugs also produced a long‐term depletion of striatal 5‐HIAA when administered alone, therefore, the changes seen after the coadministration with fenfluramine may be viewed as additive. Finally, acute PCPA pretreatment attenuated the rapid rise in 3,4‐dihydroxyphenylacetic acid (DOPAC) and homovanillic acid (homovanillic acid) induced by fenfluramine, and acute clorgyline reversed the drop in serotonin and rise in 5‐HIAA induced by fenfluramine. These results indicate that the rapid increase in dopamine activity induced by fenfluramine is partially dependent on serotonin concentration and release and that the mechanism of fenfluramine‐induced toxicity is unlike that of the other substituted amphetamines.
Single‐ and Multiple‐Dose Pharmacokinetics, Kidney Tolerability and Plasma Protein Binding of Tenoxicam in Renally Impaired Patients and Healthy Volunteers
Authors: Nilsen Odd G. , Aasarød Knut , Widerøe Tor‐Erik , Guentert Theodor W.
Published: August 2010

Abstract: The 20 mg single‐dose and 12 days repeated‐dose pharmacokinetics of tenoxicam and the 5‐OH‐tenoxicam metabolite have been evaluated in healthy volunteers and two groups of patients with different degree of renal impairment, in total 20 persons. Concomitantly, the plasma protein binding of tenoxicam and the effects of treatment on renal function were evaluated. No differences were found between the investigated groups in the pharmacokinetics of total tenoxicam and the 5‐OH metabolite did not interfere either with the pharmacokinetics or with the plasma protein binding of tenoxicam. A positive correlation was found between an increase in the free fraction (% F) of tenoxicam in plasma and a decrease in the plasma elimination half‐life in the low creatinine clearance group (40–20 ml/min.) both after the single‐dose and at steady‐state. At steady‐state, a non‐linear correlation was demonstrated between a decrease in the urinary excretion of the 5‐OH metabolite and a decrease in creatinine clearance from 130 to 20 ml/min. An increase in the plasma level of the 5‐OH metabolite by three times was found in the low creatinine clearance group as compared to healthy subjects. 14C‐Impurities of tenoxicam, as low as 1.2%, were shown to greatly influence the determination of the plasma protein binding (equilibrium dialysis) of the highly protein‐bound tenoxicam due to a non‐binding ability of the impurities to plasma proteins. No significant changes in renal parameters were found during the study. It can be concluded that the pharmacokinetics and plasma protein binding of tenoxicam and the pharmacokinetics of the 5‐OH‐tenoxicam metabolite are increasingly changed in subjects with a creatinine clearance below 40 ml/min. A decreased binding of tenoxicam to plasma proteins in low clearance patients is probably the reason for a faster elimination of tenoxicam in this group rather than a higher intrinsic hepatic metabolic activity. This study conducted in a low number of patients did not bring forward any new data indicating any adverse effects of tenoxicam on renal function.
Immunotherapy of malignant melanoma – Basic principles and novel therapeutic approaches
Authors: Enk Alexander H. , Becker Jürgen C. , Schuler Gerold
Published: August 2010

Immunotherapy has assumed increasing importance in the therapy of malignant melanoma. The main reason is the high immunogenicity of the tumor itself, so that an immune response against the tumor often exists even without immune stimulation. The goal of modern immunotherapeutic approaches is to augment these anti‐tumoral immune reactions to fight the tumor. Despite multiple successes, the ultimate breakthrough in the therapy of malignant melanoma has not yet been achieved. This overview summarizes the reasons for this lack of success and highlights future strategies for more successful therapy of malignant melanoma.
Skin toxicity of anti‐cancer therapy
Authors: Ulrich Jens , Hartmann Jörg T. , Dörr Wolfgang , Ugurel Selma
Published: August 2010

Changes in skin and its adnexa such as hair follicles and nails are among the most common side effects of antineoplastic treatments. They pose a challenge with regard to diagnostic and therapeutic aspects. This article reviews the various cutaneous reactions to chemotherapy and their most common causative agents, the adverse events of radiation therapy, as well as the characteristic skin changes under treatment with new molecular‐driven targeted agents.
Lignophenols Decrease Oleate‐Induced Apolipoprotein‐B Secretion in HepG2 Cells
Authors: Norikura Toshio , Mukai Yuuka , Fujita Shuzo , Mikame Keigo , Funaoka Masamitsu , Sato Shin
Published: August 2010

Abstract:  Lignin is one of the components in the plant cell wall, after cellulose, making up 20–30% of the global plant biomass. Lignophenols (LPs) are derivatives of lignin with high phenolic function and antioxidant properties. However, their medicinal property is not well characterised. Apolipoprotein‐B (apo‐B) is an essential component in very low‐density lipoprotein, and high levels of serum apolipoprotein‐B (apo‐B) are a major factor for coronary heart disease. In this study, we examined the effect of lignophenols on apo‐B secretion in HepG2 cells. HepG2 cells were treated with varying concentrations of LPs and 0.8 mm sodium oleate. LPs decreased oleate‐induced apo‐B secretion in a dose‐dependent manner. LPs also decreased oleate‐induced microsomal triglyceride transfer protein (MTTP) mRNA expression and cellular total cholesterol, suggesting that lipid bioavailability and lipidation of lipoprotein are likely involved in the decreased secretion of apo‐B. Furthermore, LPs decreased oleate‐induced mature sterol regulatory element binding protein 2 (SREBP‐2), a transcription factor that activates cholesterol biosynthesis. This is the first study to show that LPs can decrease oleate‐induced apo‐B secretion in HepG2 cells. The modulations of MTTP mRNA expression, cellular total cholesterol metabolism and mature SREBP‐2 expression may be important factors in the regulation of apo‐B secretion by LPs.
A Novel CC Chemokine Receptor 4 Antagonist RS‐1269 Inhibits Ovalbumin‐Induced Ear Swelling and Lipopolysaccharide‐Induced Endotoxic Shock in Mice
Authors: Nakagami Yasuhiro , Kawashima Kayo , Etori Maki , Yonekubo Kazuki , Suzuki Chie , Jojima Takaaki , Kuribayashi Takeshi , Nara Futoshi , Yamashita Makoto
Published: August 2010

Abstract:  There is growing evidence that chemokines recruit leukocytes in allergic, inflammatory and immune responses. CC chemokine receptor 4 (CCR4) is implicated as a preferential marker for T helper 2 cells, and the cells selectively respond to CC chemokine ligand 17 (CCL17) and CCL22. We searched for compounds having a profile as a CCR4 antagonist from an in‐house library and have previously reported that 3‐{2‐[(2R)‐2‐phenyl‐4‐(4‐pyridin‐4‐ylbenzyl)morpholin‐2‐yl]ethyl}quinazoline‐2,4(1H,3H)‐dione (named RS‐1154) was capable of significantly inhibiting the binding of [125I]CCL17 to human CCR4‐expressing CHO cells. From further synthesis of its derivatives, we newly focused on 3‐(isobutyrylamino)‐N‐{2‐[(2R)‐2‐phenyl‐4‐(4‐pyridin‐4‐ylbenzyl)morpholin‐2‐yl]ethyl}benzamide (RS‐1269), which showed potency comparable to RS‐1154 in inhibiting CCL17‐induced migration of DO11.10 mice‐derived T helper 2 cells with an IC50 value of 5.5 nM in vitro. We then investigated the pharmacological effects of RS‐1269 on ovalbumin‐induced ear swelling and lipopolysaccharide‐induced endotoxic shock in mice. The ear thickness was significantly decreased by oral administration of RS‐1269 at the dose of 30 mg/kg. Treatment with lipopolysaccharide significantly increased the serum level of tumour necrosis factor‐α. Compared with an anti‐CCL17 antibody, RS‐1269 significantly inhibited the production at the dose of 100 mg/kg. These results raise the possibility that RS‐1269 or one of its derivatives has potential to serve as a prototype compound to develop therapeutic agents for atopic dermatitis and inflammatory diseases.
Australian food regulations public consultation process: Teaching postgraduate dietetics students to participate
Authors: Somerset Shawn
Published: August 2010

Objective:  To assess a teaching strategy to develop competency, familiarity and willingness of dietetic students to participate in food regulation development.

Design:  Qualitative evaluation of self‐perceived learning outcomes.

Subjects/Setting:  Two consecutive cohorts (n = 39) of postgraduate dietetics students from Griffith University.

Intervention:  Preparation and presentation of a formal response to a call for comment by Australia's food regulatory body (Food Standards Australia New Zealand) during the period 1999–2001.

Main outcome measures:  Self‐reported descriptions of confidence, familiarity and willingness to participate in the public consultation process.

Results:  Following the assignment, students generally reported being more familiar with the regulatory process and more confident to participate. Most students identified the importance of reference material on Food Standards Australia New Zealand procedures that they could use for review should the opportunity for participation arise at a later date. A major issue identified was the potential for cynicism towards the process. This issue was seen as a potential barrier to participation by students after graduation.

Applications/Conclusions:  This issues‐based approach to teaching of a food regulation system has potential to enhance participation in regulatory development by a broader cross‐section of dietitians.
Vitamin D deficiency in Australia and New Zealand: What are the dietary options?
Authors: SHRAPNEL William , TRUSWELL Stewart
Published: August 2010

Measurement of serum vitamin D levels in population samples has revealed unexpectedly high prevalence of vitamin D deficiency among children, adults, the elderly and other vulnerable groups in Australia and New Zealand. The new Nutrient Reference Values report has established dietary recommendations for vitamin D of between 5 and 15 µg/day, depending on age. Dietary intakes of vitamin D in Australia typically fall in the range of 2–3 µg/day, below intakes in comparable countries. Dietary intake of vitamin D is currently dependent on consumption of a few key foods, notably margarine and oily fish. Current models of healthy eating do not deliver the recommended amounts of vitamin D and need review. Consideration should be given to the range of foods fortified with vitamin D, which is currently limited. Higher dietary intakes of vitamin D in overseas countries have been achieved through the fortification of margarine, milk and breakfast cereals. Increased voluntary fortification of dairy products with vitamin D would be a safe and simple means of increasing vitamin D intakes in Australasia in the short term. The relatively high dietary recommendation for vitamin D for elderly people cannot be met through the existing food supply and supplementation appears to be a desirable option for many.
Depression: Does nutrition have an adjunctive treatment role?
Authors: VOLKER Dianne , NG Jade
Published: August 2010

Depression is a serious illness, affecting more than one million Australians each year. It causes significant morbidity and is a major risk factor for deliberate self‐harm and suicide. Depression was traditionally viewed as a personality weakness, for which few treatment options were available. The simplistic view that depression is a personality weakness has changed in recent times. Depression is now widely recognised as a mood disorder with underlying biological (biochemical and genetic) and psychosocial causes and as such is responsive to a number of different treatments. The aim of the present paper is to review the literature related to dietary manipulation and how manipulation may assist in treating this illness. Evidence reviewed supports a potential therapeutic benefit of n‐3 polyunsaturated fatty acids for the alleviation of negative symptoms associated with depression. Omega‐3 polyunsaturated fatty acids, optimal omega balance, folate, tryptophan, vitamin B6, B12, S‐adenosyl‐L‐methionine and Hypericum perforatum may all serve as adjuncts to psychosocial and pharmacological therapies, with positive implications for long‐term prognosis.
Effects of Personality Style, Anxiety, and Depression on Reported Reasons for Smoking1
Authors: Scheitrum Raquel R. , Akillas Emmanuel
Published: August 2010

This study examined the effects of personality style, anxiety, and depression on the reasons for smoking reported by active smokers. Type A individuals with high trait anxiety viewed smoking as a way to stimulate themselves, whereas Type B individuals claimed that they smoked in order to relax. No such relationship was found for smokers who were not anxious. Smokers who had a high degree of depressive symptomatology were more likely to smoke for stimulation than were smokers with a low degree of depressive symptomatology. These results support Warburton's theory (1988) that smoking is an active coping strategy maintained through nicotine's psychological benefits.
Prejudice Toward People With Cancer or AIDS: Applying the Integrated Threat Model
Authors: Berrenberg Joy L. , Finlay Krystina A. , Stephan Walter G. , Stephan Cookie
Published: August 2010

Two experiments applied the integrated threat theory of prejudice to predicting attitudes toward people with terminal cancer or AIDS. The measures, which were designed to assess the components of the model (realistic threats, symbolic threats, inter group anxiety, and negative stereotypes), were reliable and generally predictive of attitudes. The theory predicted attitudes toward AIDS better than attitudes toward cancer, perhaps because more people believe that they are likely to become a member of the cancer out‐group. The benefits of applying social psychological theory to health issues are discussed along with suggestions for future research.
Self‐Efficacy Predicts Physical Activity in Individuals With Fibromyalgia1
Authors: Culos‐Reed S. Nicole , Brawley Lawrence R.
Published: August 2010

The purpose of the current study was to prospectively examine the relationship between physical activity patterns and psychosocial predictors in a sample of individuals with fibromyalgia (FM). Individuals with FM (N= 61) tracked their physical activity over a 1 ‐month period and completed baseline and endpoint questionnaires. Self‐efficacy provided the framework for the investigation, with both self‐efficacy and intention examined as predictors of physical activity. Exploratory analyses examined the addition of attitude and social influence as predictors of intention and behavior. The results supported the importance of self‐efficacy as a direct prospective predictor of the physical activity of FM individuals. Future research should examine whether maintaining strong intentions is helpful or realistic in motivating physical activity as a treatment option for individuals with FM.
Anxiety and Depression: Congruent, Separate, or Both?1
Authors: Endler Norman S. , Macrodimitris Sophia D. , Kocovski Nancy L.
Published: August 2010

This study investigated whether using state‐trait distinctions of both depression and anxiety would allow for further identification of the unique and overlapping features of these two symptom structures. Three hundred and seventy‐one undergraduate students (122 men, 249 women) responded to questionnaires exploring both state and trait depression and anxiety. Results revealed that women reported higher levels of depression and anxiety for all measures except for state anxiety, where men scored higher than women. Results also demonstrated stronger within‐construct correlations (i.e., state depression with trait depression) than between construct correlations (i.e., state depression with trait anxiety), supporting the distinctness of the two constructs. The uniqueness of depression and anxiety was further supported by factor analysis. Overlap in symptoms also occurred, but the correlations were generally stronger for congruent symptom types (i.e., state depression and state anxiety rather than state depression and trait anxiety). Results are discussed in terms of viewing depression and anxiety as distinct constructs with overlapping features.
Breast Cancer Detection in Asymptomatic Women: Health Beliefs Implicated in Secondary Prevention
Authors: Umeh Kanayo , Dimitrakaki Vithleem
Published: August 2010

This study assessed the usefulness of health belief model (HBM) constructs in predicting the frequency and proficiency of breast self‐examination among Greek women. Both additive and multiplicative functions were tested. Cross‐sectional data from 195 women were analyzed. Health beliefs explained 16.5% and 19.7% of the variance in frequency and proficiency, respectively. Frequent and proficient breast examination was associated with fewer perceived barriers. Moreover, elevated confidence and susceptibility estimates predicted greater frequency and proficiency, respectively. One moderator interaction emerged, but this was attenuated after accounting for other health beliefs. These findings provide qualified support for the HBM and present a useful template for developing interventions to promote secondary prevention.
Physical Activity and Social Physique Anxiety in Older Women: The Moderating Effects of Self‐Presentation Efficacy
Authors: Woodgate Jennifer , Ginis Kathleen A. Martin , Sinden Adrienne R.
Published: August 2010

Given the inconsistent relationships observed between social physique anxiety (SPA) and physical activity, it is possible that other variables moderate this relationship. This study examined self‐presentation efficacy (SPE) as a potential moderator. Participants were 81 older women. Multiple regression analysis revealed that SPA, SPE, and the SPA x SPE interaction significantly predicted physical activity, with the SPA x SPE interaction explaining 6% of the variance in activity. Evaluation of this interaction indicated that SPA was negatively correlated with activity only for women with high and mean SPE and was unrelated to activity for women with low SPE. These findings suggest that, for older women, lower levels of SPA are not always related to greater activity. Rather, SPE is an important moderator of the SPA‐physical activity relationship.
Academic Study, College Examinations, and Stress: Issues in the Interpretation of Cardiovascular Reactivity Assessments With Student Participants1
Authors: Hughes Brian M.
Published: August 2010

Stress arising from academic performance affects many college students. Moreover, students account for the majority of participants in cardiovascular reactivity research. The current research comprised three brief experiments investigating different aspects of student samples. In Experiment 1, students' (n = 30) academic fear of failure was found to be negatively correlated with systolic blood pressure reactivity. In Experiment 2, students' (n= 13) blood pressure was found to be significantly elevated 2 weeks before college examinations, compared with postexamination levels. Finally, in Experiment 3, students' (n = 19) examination performance was positively correlated with preexamination cardiovascular reactivity. These findings suggest specific college‐related factors that influence the cardiovascular stress response in students and, therefore, should aid the interpretation of much research conducted in cardiovascular health psychology.
Depression and Antidepressant Use in Gastrointestinal Carcinoid Cancer Patients1
Authors: Soliday Elizabeth , Garofalo John P. , Smith Suzanne R. , Warner Richard R. P.
Published: August 2010

Although mood disturbance is a common manifestation in all cancers that require clinical attention, very little is known regarding the psychiatric management of depression in patients with gastrointestinal carcinoid tumors. The goal of this study was to evaluate the degree of depression among patients with gastrointestinal carcinoid tumors, determine the prevalence of selective serotonin reuptake inhibitor (SSRI) use among these patients, and determine whether SSRI users differed from nonusers on demographic and general medical variables. Approximately 22% of the respondents in this study met screening criteria for clinically elevated or borderline depression. Moreover, 7% of respondents were following an SSRI regimen, whereas 7% were following a non‐SSRI antidepressant regimen. Analyses revealed no differences on demographic or general medical indicators between SSRI users and nonusers.
An Analysis of Peer Influence and Peer Selection on Human Immunodeficiency Virus Risk Behaviors1
Authors: Brown Victoria L. , Trevino Roberto A. , Richard Alan J. , Bell David C. , Montoya Isaac D. , Brown H. Shelton
Published: August 2010

Much of the public health literature indicates that peers have a significant effect on risky health behaviors. However, these studies have not considered the role of peer endogeneity (i.e., peer selection). Thus, the purpose of this study is to ascertain the importance of considering peer endogeneity when discussing the consequences of peer behavior on individual behavior, particularly on risky sexual behavior. The results show a nonsignificant association between perceived peer support for condom use and actual individual condom use in this sample of low‐income, high‐risk individuals. More notably, however, the results point to the importance of considering peer endogeneity in any estimation of peer influence on risky health behaviors.
Do Ethical Principles Explain Moral Norm? A Test for Consent to Organ Donation
Authors: Blondeau Danielle , Godin Gaston , Gagnéa Camille , Martineau Isabelle
Published: August 2010

Moral norm is a strong predictor of intention with respect to certain behaviors. In the context of a study of organ donor consent, the goal was to enrich the ethics construct with the help of the following three dimensions: autonomy, beneficence, and justice. The results indicated that theinterrelations among the ethics variables were significant. However, the results also indicated that moral norm was influenced only by beneficence. Conducting other studies in different cultural contexts and verifying other behaviors would shed light on whether beneficence still influences moral norm.
The Embeddedness of Body Image: A Study of Women With and Without Eating Disorders
Authors: Lewis Vivienne , Donaghue Ngaire
Published: August 2010

Body image and its relationship to women's well‐being has been researched extensively partially because of its links with dangerous dieting behaviors. However, research has been limited to investigating specific aspects of self‐concept and has failed to look at beliefs about the body in the more specific context of women's lives. The study extended research by examining the interaction between body image, goal striving, and well‐being in a clinical and nonclinical sample. It was hypothesized that the extent to which body image is a main goal in a woman's life and the extent to which she sees it to be related to striving for other life goals (embeddedness) would influence how strongly body dissatisfaction impacts on her well‐being. Women (N= 161) completed a questionnaire. Results indicated that embeddedness of body image moderated the relationship between body and life satisfaction for all women and that this effect was consistent over a 3‐month follow‐up. Clinical differences were found. Results highlight the importance of seeing body image in the context of women's lives, not just for those with eating disorders but for those without. Suggestions for therapeutic intervention are made.
Relationship Between Interindividual Differences and Physiological Indexes of Acute Stress in Rats
Authors: Nagane Mitsuo , Nomura Masahiko
Published: August 2010

We used in vivo microdialysis to examine interindividual differences in the effects of acute immobilization stress and diazepam treatment on monoamine turnover in the hippocampus of male rats as an index of stress. Immobilization significantly increased the concentrations of 3,4‐dihydroxyphenyl‐aceticacid (DOPAC), homovanillic acid (HVA), and 5‐hydroxyindoleacetic acid (5‐HIAA). This effect was attenuated by injection of diazepam, Interindividual differences in reactivity to stressors caused differential changes in different metabolic products of monoamines. In our study, stress‐induced changes in DOPAC levels were relatively great, and there was a similar change in the concentration of HVA. We conclude that at least 2 indexes of stress should be measured to take into account interindividual differences in the changes in stress indexes.
Social Support as a Moderator of the Big‐Fish‐in‐a‐Little‐Pond Effect in Online Self‐Help Support Groups1
Authors: Bane Cynthia M. H. , Haymaker Christopher M. B. , Zinchuk Jessica
Published: August 2010

Downward social comparisons to others in a relatively unsuccessful group can bolster mood, a phenomenon known as the big‐fish‐in‐a‐little‐pond effect (BFLPE). The current study examined social support as a moderator of the BFLPE in online weight‐management support groups (SGs). Participants (N= 149) were recruited from weight‐management message boards. In an Internet survey, participants made weight‐related social comparisons to the average person and the average SG member. Big fish indicated that they would feel more self‐pride after reading a downward social comparison message than did other participants, but the BFLPE occurred only for participants with lower weight‐related social support. Social support could foster collective identity in online self‐help support groups, reducing the BFLPE.
Can a 15‐Hour (Overnight) Urinary Catecholamine Measure Substitute for a 24‐Hour Measure?1
Authors: Janicki‐Deverts Denise , Zilles Kelly , Cohen Sheldon , Baum Andrew
Published: August 2010

This study examined whether 15‐hr and 24‐hr urinary catecholamine measures show comparable associations with other physiological measures that are expected to correlate with sympathetic nervous system activity. Participants (193 healthy adults) provided 24‐hr urine samples that were collected in a controlled environment (hotel), and divided into 9‐hr daytime and 15‐hr overnight collections. On the same day, resting blood pressure (BP) was measured, and 8 samples of salivary Cortisol were collected. Catecholamine (15‐hr and 24‐hr) measures were correlated substantially in the entire sample, and when examined separately by sex and by race. Both 15‐hr and 24‐hr epinephrine (E) correlated significantly with systolic BP and Cortisol; 15‐hr and 24‐hr norepinephrine (NE) correlated significantly with Cortisol. Correlation coefficients for 15‐hr measures were similar, but not equivalent to those for 24‐hr measures. Urinary catecholamines obtained via 15‐hr overnight collection approximated but were not equivalent to catecholamines obtained via 24‐hr collection. Overnight collection was associated with reduced power to detect significant associations of catecholamines with criterion variables, such that use of 15‐hr rather than 24‐hr sampling required a relative increase in sample size of 1.32 times for E and 1.18 times for NE to detect similar effects. Researchers should weigh the costs of additional subjects to the benefit of decreased burden when choosing between the two sampling methods.
“It's Who I Am … Really!’ The Importance of Integrated Regulation in Exercise Contexts1
Authors: Wilson Philip M. , Rodgers Wendy M. , Loitz Christina C. , Scime Giulia
Published: August 2010

The purpose of this series of studies was to evaluate a measure of integrated regulation specific to exercise contexts in line with Self‐Determination Theory (SDT; Deci & Ryan, 1985, 2002). To address this purpose, three studies were conducted to test select psychometric and theoretical properties of four integrated regulation items created for use within the Behavioural Regulation in Exercise Questionnaire (BREQ). Confirmatory factor analyses conducted in Studies 1 and 2 supported the inclusion of integrated regulation within the expanded BREQ measurement model. Simultaneous multiple regression analyses (SMRAs) conducted in Study 2 indicated that greater need satisfaction promoted endorsement of autonomous exercise motives, including integrated regulation. Finally, SMRA conducted in Study 3 revealed that integrated regulation contributed to the prediction of exercise behavior and physical self‐worth. Collectively, the results of this investigation suggest that the new integrated regulation items can be used in conjunction with the BREQ without compromising validity, and support Deci and Ryan's (1985, 2002) assertions regarding the importance of autonomous extrinsic motives, including integrated regulation in exercise domains.