bluuebunny/crossref_metadata_2025_split huggingface dataset:
Characterisation of the binding of [3H]‐SB‐674042, a novel nonpeptide antagonist, to the human orexin‐1 receptor
Authors: Langmead Christopher J , Jerman Jeffrey C , Brough Stephen J , Scott Claire , Porter Rod A , Herdon Hugh J 
Published: January 2004

This study characterises the binding of a novel nonpeptide antagonist radioligand, [3H]SB‐674042 (1‐(5‐(2‐fluoro‐phenyl)‐2‐methyl‐thiazol‐4‐yl)‐1‐((S)‐2‐(5‐phenyl‐(1,3,4)oxadiazol‐2‐ylmethyl)‐pyrrolidin‐1‐yl)‐methanone), to the human orexin‐1 (OX1) receptor stably expressed in Chinese hamster ovary (CHO) cells in both a whole cell assay and in a cell membrane‐based scintillation proximity assay (SPA) format.
Specific binding of [3H]SB‐674042 was saturable in both whole cell and membrane formats. Analyses suggested a single high‐affinity site, with Kd values of 3.76±0.45 and 5.03±0.31 nM, and corresponding Bmax values of 30.8±1.8 and 34.4±2.0 pmol mg protein−1, in whole cell and membrane formats, respectively. Kinetic studies yielded similar Kd values.
Competition studies in whole cells revealed that the native orexin peptides display a low affinity for the OX1 receptor, with orexin‐A displaying a ∼five‐fold higher affinity than orexin‐B (Ki values of 318±158 and 1516±597 nM, respectively).
SB‐334867, SB‐408124 (1‐(6,8‐difluoro‐2‐methyl‐quinolin‐4‐yl)‐3‐(4‐dimethylamino‐phenyl)‐urea) and SB‐410220 (1‐(5,8‐difluoro‐quinolin‐4‐yl)‐3‐(4‐dimethylamino‐phenyl)‐urea) all displayed high affinity for the OX1 receptor in both whole cell (Ki values 99±18, 57±8.3 and 19±4.5 nM, respectively) and membrane (Ki values 38±3.6, 27±4.1 and 4.5±0.2 nM, respectively) formats.
Calcium mobilisation studies showed that SB‐334867, SB‐408124 and SB‐410220 are all functional antagonists of the OX1 receptor, with potencies in line with their affinities, as measured in the radioligand binding assays, and with approximately 50‐fold selectivity over the orexin‐2 receptor.
These studies indicate that [3H]SB‐674042 is a specific, high‐affinity radioligand for the OX1 receptor. The availability of this radioligand will be a valuable tool with which to investigate the physiological functions of OX1 receptors.

British Journal of Pharmacology (2004) 141, 340–346. doi:10.1038/sj.bjp.0705610
Contribution of nitric oxide produced by inducible nitric oxide synthase to vascular responses of mesenteric arterioles in streptozotocin‐diabetic rats
Authors: Ishikawa Tomohisa , Kohno Fumika , Kawase Ryosuke , Yamamoto Yuri , Nakayama Koichi 
Published: January 2004

The functional changes in mesenteric arterioles of streptozotocin‐induced diabetes were investigated by intravital microscopy. The mesentery was exteriorized from anesthetized rats, spread in a chamber, and superfused with Tyrode solution. All drugs tested were applied to the superfusing Tyrode solution.
Compared with age‐matched controls, the diabetic rats showed enhanced vascular sensitivity to phenylephrine, an α1‐adrenoceptor agonist. The preincubation of the mesentery with NG‐nitro‐L‐arginine (L‐NNA), a nitric oxide synthase (NOS) inhibitor, shifted the phenylephrine‐concentration–response curves to the left in both the diabetic and control rats. Even in the presence of L‐NNA, the sensitivity to phenylephrine was higher in the diabetic rats than in the control.
Acetylcholine relaxed the mesenteric arterioles in both groups, but to a significantly greater extent in the control than in the diabetic rats. However, the L‐NNA‐induced constriction of arterioles did not differ significantly between the groups. In contrast, the amplitude of the constrictions of mesenteric arterioles induced by S‐ethylisothiourea, an inducible NOS (iNOS) inhibitor, was significantly greater in the diabetic rats than in the control.
Immunostaining of the mesentery with a specific antibody for iNOS revealed iNOS in the microvessels of only the diabetic rats.
These results suggest that constrictor responses to α1‐adrenoceptor stimulation are sensitized in the mesenteric arterioles of STZ‐diabetic rats, and that iNOS expressed in the arteriolar smooth muscle plays a role in suppressing the basal tone and the reactivity of the arterioles in STZ‐diabetic rats.

British Journal of Pharmacology (2004) 141, 269–276. doi:10.1038/sj.bjp.0705611
Minoxidil opens mitochondrial KATP channels and confers cardioprotection
Authors: Sato Toshiaki , Li Yulong , Saito Tomoaki , Nakaya Haruaki 
Published: January 2004

ATP‐sensitive potassium channel in the mitochondrial inner membrane (mitoKATP channel) rather than in the sarcolemma (sarcKATP channel) appears to play an important role in cardioprotection. We examined the effect of minoxidil, a potent antihypertensive agent and hair growth stimulator, on sarcKATP and mitoKATP channels in guinea‐pig ventricular myocytes.
Minoxidil activated a glybenclamide‐sensitive sarcKATP channel current in the whole‐cell recording mode with an EC50 of 182.6 μM. Minoxidil reversibly increased the flavoprotein oxidation, an index of mitoKATP channel activity, in a concentration‐dependent manner. The EC50 for mitoKATP channel activation was estimated to be 7.3 μM; this value was notably ∼25‐fold lower than that for sarcKATP channel activation.
Minoxidil (10 μM) significantly attenuated the ouabain‐induced increase of mitochondrial Ca2+ concentration, which was measured by loading cells with rhod‐2 fluorescence. Furthermore, pretreatment with minoxidil (10 μM) before 20‐min no‐flow ischaemia significantly improved the recovery of developed tension measured after 60 min of reperfusion in coronary perfused guinea‐pig ventricular muscles. These cardioprotective effects of minoxidil were completely abolished by the mitoKATP channel blocker 5‐hydroxydecanoate (500 μM).
Our results indicate that minoxidil exerts a direct cardioprotective effect on heart muscle cells, an effect mediated by the selective activation of mitoKATP channels.

British Journal of Pharmacology (2004) 141, 360–366. doi:10.1038/sj.bjp.0705613
Effects of chloride channel blockers on hypotonicity‐induced contractions of the rat trachea
Authors: Coelho Roberta R , Souza Emmanuel P , Soares Pedro M G , Meireles Ana Vaneska P , Santos Geam C M , Scarparo Henrique C , Assreuy Ana Maria S , Criddle David N 
Published: January 2004

We have investigated the inhibitory effects of blockers of volume‐activated (Clvol) and calcium‐activated (ClCa) chloride channels on hypotonic solution (HS)‐induced contractions of rat trachea, comparing their effects with those of the voltage‐dependent calcium channel (VDCC) blocker nifedpine.
HS elicited large, stable contractions that were partially dependent on the cellular chloride gradient; a reduction to 41.45±7.71% of the control response was obtained when extracellular chloride was removed. In addition, HS‐induced responses were reduced to 26.8±5.6% of the control by 1 μM nifedipine, and abolished under calcium‐free conditions, indicating a substantial requirement for extracellular calcium entry, principally via VDCCs.
The established Clvol blockers tamoxifen (10 μM) and 4,4′‐diisothiocyanatostilbene‐2,2′‐disulphonic acid (1–100 μM), at concentrations previously reported to inhibit Clvol in smooth muscle, did not significantly inhibit HS‐induced contractions.
In contrast, the recognized ClCa blocker niflumic acid (NFA; 1–100 μM) produced a reversible, concentration‐dependent inhibition of HS responses, with a reduction to 36.6±6.4% of control contractions at the highest concentration. The mixed Clvol and ClCa blocker, 5‐nitro 2‐(3‐phenylpropylamine) benzoic acid (NPPB; 10–100 μM) also elicited concentration‐related inhibition of HS‐induced contractions, producing a decrease to 35.9±11.3% of the control at 100 μM.
Our results show that HS induces reversible, chloride‐dependent contractions of rat isolated trachea that were inhibited by NFA and NPPB, while exhibiting little sensitivity to recognized blockers of Clvol. The data support the possibility that opening of calcium‐activated chloride channels under hypotonic conditions in respiratory smooth muscle may ultimately lead to VDCC‐mediated calcium entry and contraction.

British Journal of Pharmacology (2004) 141, 367–373. doi:10.1038/sj.bjp.0705615
Type, extent and use of colours in ready‐to‐eat (RTE) foods prepared in the non‐industrial sector – a case study from Hyderabad, India
Authors: Jonnalagadda Padmaja R. , Rao Pratima , Bhat Ramesh V. , Nadamuni Naidu A. 
Published: February 2004

SummaryThe type and extent of colours added to ready‐to‐eat (RTE) foods prepared in the non‐industrial sector of India was investigated. Of the 545 RTE foods analysed, 90% contained permitted colours, 2% contained a combination of permitted and non‐permitted colours and 8% contained only non‐permitted colours. However in RTE foods with permitted colours, 73% exceeded 100 ppm, as prescribed by the Prevention of Food Adulteration Act of India, and 27% were within the prescribed levels. Among the permitted colours, tartrazine was the most widely used colour followed by sunset yellow. The maximum concentration of colours was detected in sweet meats (18 767 ppm), non‐alcoholic beverages (9450 ppm), miscellaneous foods (6106 ppm) and hard‐boiled sugar confectioneries (3811 ppm). Among the non‐permitted colours found, rhodamine was most commonly used. Some of the foods, such as savouries and miscellaneous foods like sugar coated aniseed and almond milk, are not supposed to contain colours as per the Prevention of Food Adulteration Act, but were found to contain colours.
Under- and overreporting of energy is related to obesity, lifestyle factors and food group intakes in Jamaican adults
Authors: Mendez Michelle A , Wynter Suzanne , Wilks Rainford , Forrester Terrence 
Published: January 2004

AbstractObjective:Research in industrialised countries has documented a high prevalence of underreported energy intakes associated with characteristics such as obesity. This paper examines the prevalence, patterns and impact of energy under- and overreporting on diet–obesity relationships in a middle-income developing country.Design:A 70-item food-frequency questionnaire was used. Underreporters had reported energy intakes < 1.35 × basal metabolic rate (BMR), overreporters > 2.4 × BMR. Multinomial models were used to identify characteristics associated with implausible reporting. Intakes were compared across reporting groups to assess evidence of bias. Associations between diet and obesity were compared with and without adjustment for implausible reporting.Setting:Spanish Town, neighbouring the capital city of Kingston, Jamaica.Subjects:Eight hundred and ninety-one Jamaican adults, aged 25–75 years, were randomly recruited.Results:More women than men (38.6% vs. 22.5%) underreported, but more men overreported energy (23.7% vs. 16.0%). Underreporting was positively associated with obesity, special diets, smoking and age; age was inversely associated with overreporting. Underreporters estimated lower energy from potentially socially undesirable food groups (e.g. snacks) and higher intakes of ‘healthy’ foods (e.g. fruit) than did plausible reporters. For some of these food groups, significant differences in intakes among normal-weight versus obese subjects observed among plausible reporters were absent when implausible reporters were included. In models of food group–obesity associations, adjusting for implausible energy yielded more credible results that more closely resembled findings in plausible reporters.Conclusions:Energy under- and overreporting are highly prevalent in Jamaica. Adjusting for implausible reporting may help to reduce bias in diet–health outcome associations.
Having lunch at a staff canteen is associated with recommended food habits
Authors: Roos Eva , Sarlio-Lähteenkorva Sirpa , Lallukka Tea 
Published: January 2004

AbstractObjective:To describe the characteristics of employees having lunch at staff canteens and to examine the association between workplace lunch and recommended food habits.Design:A mailed questionnaire including data on lunch pattern, food habits, sociodemographic background, work-related factors and body weight. Logistic regression models including food habits as dependent variables and lunch pattern, sociodemographic factors, work-related factors and body mass index as independent variables.Setting:Helsinki Health Study survey data, collected in spring 2001.Subjects:Employees from the City of Helsinki reaching 40, 45, 50, 55 and 60 years. The data included 2474 women and 591 men; the response rate was 68%.Results:About half of those with a staff canteen at work had lunch there. Those with higher educational level were more likely to have lunch at the staff canteen, as also were women with pre-school children and normal-weight men. Those having lunch at staff canteens were more likely to follow recommended food habits, compared with other subjects. Having lunch at the staff canteen seemed to increase the consumption frequency of vegetables and fish.Conclusions:Having lunch at staff canteens is associated with the quality of the diet. To serve a cooked meal including vegetables during working time may be an efficient way to improve diet among adult employees. More emphasis should be put on increasing the possibility for employees to have lunch at staff canteens.
Energy-dense diets are associated with lower diet costs: a community study of French adults
Authors: Darmon Nicole , Briend André , Drewnowski Adam 
Published: January 2004

AbstractObjective:High consumption of energy-dense foods has been linked to high energy intakes and excess weight gain. This study tested the hypothesis that high energy density of the total diet is associated with lower diet costs.Design:Dietary intakes of 837 French adults, aged 18–76 years, were assessed using a dietary history method. Dietary energy density (MJ kg−1) was calculated by dividing total energy by the edible weight of foods consumed. Daily diet cost (€day−1) was estimated using mean national food prices for 57 food items. The relationship between dietary energy density and diet cost at each level of energy intake was examined in a regression model, adjusted for gender and age.Results:The more energy-dense refined grains, sweets and fats provided energy at a lower cost than did lean meats, vegetables and fruit. Within each quintile of energy intake, diets of lower energy density (MJ kg−1) were associated with higher diet costs (€day−1).Conclusion:In this observational study, energy-dense diets cost less whereas energy-dilute diets cost more, adjusting for energy intakes. The finding that energy-dilute diets are associated with higher diet costs has implications for dietary guidelines and current strategies for dietary change.
Determinants of diet quality
Authors: Thiele Silke , Mensink Gert BM , Beitz Roma 
Published: January 2004

AbstractBackground:An unbalanced diet is a main risk factor for several chronic diseases. This paper identifies groups of individuals with an unbalanced diet based on the consumption of nutrients. A characterisation of the groups may help to focus efforts aimed at improving the dietary behaviour of the population.Methods:Using nutritional data of 1763 men and 2267 women participating in the German Nutrition Survey of 1998, we constructed two indices for diet quality that each combines a large amount of nutrients into a single indicator. The impact of sociodemographic and lifestyle characteristics on the diet quality indices was analysed using multiple regression analyses.Results:The results show a considerable variation of diet quality between different groups of individuals. High diet quality in terms of the consumption of vitamins, minerals and trace elements is positively associated with income, education level, age, energy intake, food diversity, sport activity and vegetarianism. On the other hand, a low diet quality as indicated by high intakes of e.g. fat, sugar, alcohol and sodium can be expected when energy intake is high, for individuals of middle age and for pregnant and breast-feeding women.Conclusion:The results of this study help to identify groups of individuals with preferable and non-preferable diet quality. For developing public health strategies, in particular the impact of age on diet quality seems to be interesting. The rising diet quality with increasing age could reflect a changing health consciousness. It could thus be a challenge for health policy to promote a healthy way of living focused especially on young individuals.
Assessment of the nutritional risk of > 53-year-old men and women in Taiwan
Authors: Tsai Alan C , Chang Jack MC , Lin Harvey , Chuang Yi-Li , Lin Shu-Hui , Lin Yu-Hsuan 
Published: January 2004

AbstractObjective:The study was conducted to gain an understanding of the status of potential nutrition risks in > 53-year-old men and women in Taiwan.Methods:The study employed a validated nutrition-risk screening questionnaire, the Mini Nutritional Assessment, to assess the potential risk of undernutrition in the elderly population in Taiwan. The questionnaire was translated into the local language, Chinese, and was modified slightly based on cultural considerations. It was administered to 4440 randomly selected subjects by means of face-to-face interviews. The questionnaire included questions on subjective self-evaluations, global parameters, simple dietary assessment and some anthropometric measurements.Results:Results show that the questionnaire can be used effectively as a tool to screen for individuals who are at risk of undernutrition. It showed that the proportion of the elderly population at risk of nutritional inadequacy is relatively low, but does increase with advanced ageing. The proportion of the elderly considered at high risk of undernutrition was found to increase with age, ranging from 0.88% for 53–60-year-old subjects to 1.86% for subjects aged 60–70 years, 3.6% for 70–80-year-olds and 5.3% for >80-year-old subjects.Conclusion:The study showed that a simple questionnaire adopted from the Mini Nutritional Assessment can be employed to provide a preliminary screening and to identify individuals who are potentially at increased risk of nutritional inadequacy in the elderly population in Taiwan.
Use of the 70‐Degree Diamond Burr in the Management of Complicated Frontal Sinus Disease
Authors: Chandra Rakesh K. , Schlosser Rodney , Kennedy David W. 
Published: January 2004

AbstractObjectives/Hypothesis: Management of frontal sinus disease may require drill‐out of bone in the frontal recess for access, ventilation, and drainage of the sinus cavity; removal of osteitic foci; or resection of neoplastic tissue. Technological advances, particularly burrs with angles of 70 degrees and stereotactic navigational imaging, offer new opportunities to provide access and minimize trauma. The preliminary study evaluates the safety and efficacy of such minimally invasive approaches.Study Design: Retrospective review.Methods: The authors describe the use of a 70‐degree diamond burr in a series of 10 patients with complicated frontal sinus disease who underwent endoscopic frontal sinusotomy under stereotactic imaging guidance.Results: The diagnoses consisted of frontal sinus mucocele (n = 4), chronic frontal sinusitis (n = 1), Pott's puffy tumor after frontoethmoid fracture (n = 1), and recurrent inverting papilloma (n = 4). Partial septectomy was required in 6 of 10 patients. No complications were attributable to the drill‐out procedure, despite a pre‐existing frontoethmoid bony dehiscence in 6 of 10 patients. One patient had a CSF leak during removal of tumor from the skull base. One patient required revision frontal sinusotomy 10 months after the initial procedure, and another required further surgery for residual inverting papilloma on the medial orbital wall. All frontal sinusotomies were patent at last follow‐up (mean period, 9.3 mo).Conclusion: Extended endoscopic frontal sinusotomy may be necessary in the management of complicated frontal sinus inflammatory disease and inverting papilloma. The 70‐degree diamond burr is a safe and effective tool for access to the frontal recess. Complication rates appear to be similar to those for other extended frontal sinusotomy approaches.
Propofol Decreases Waste Anesthetic Gas Exposure During Pediatric Bronchoscopy
Authors: Zestos Maria M. , Bhattacharya Debashish , Rajan Sankar , Kemper Sharon , Haupert Michael 
Published: January 2004

AbstractObjective: This study compared the anesthetic gas exposure and operating conditions during insufflation anesthesia with halothane‐alone versus halothane‐propofol in children undergoing direct laryngobronchoscopy.Study Design: Forty‐six children were enrolled in this randomized prospective study, with institutional review board approval and informed consent.Methods: All children were anesthetized by halothane mask induction and anesthesia was maintained using spontaneous ventilation with insufflation. No muscle relaxants or opioids were used. In the halothane group, halothane was titrated as needed. In the propofol group, halothane was decreased to 1% inspired concentration and the propofol was titrated as needed to maintain spontaneous ventilation and a still patient. Trace anesthetic gases, hemodynamic stability, and operating conditions were measured.Results: The groups were similar in age, weight, and bronchoscopy time. There was significantly less gas exposure in the propofol group (25 ± 33 parts per million) versus the halothane group (66 ± 97 ppm; P < .02). There was a trend toward earlier emergence in the halothane group (33 ± 13 minutes) versus the propofol group (41 ± 17 minutes). Postoperative stridor was common, occurring in 30% of children.Conclusions: Insufflation anesthesia with spontaneous respiration provides excellent surgical conditions for laryngobronchoscopy. The addition of propofol resulted in fewer airway complications (P = .047). Although the addition of propofol significantly decreased anesthetic gas exposure in the operating room, both techniques resulted in operating room pollution that exceeded the maximum levels of 2 ppm per hour recommended by the US National Institute for Occupational Safety and Health (NIOSH).
Vestibular Nerve Section Versus Intratympanic Gentamicin for Meniere's Disease
Authors: Hillman Todd A. , Chen Douglas A. , Arriaga Moises A. 
Published: January 2004

AbstractObjectives/Hypothesis:Vestibular nerve section and transtympanic gentamicin administration are procedures with proven efficacy in the treatment of vertigo associated with Meniere's disease refractory to medical management. Hearing loss is a known complication of each of these procedures; however, there has not been a report of hearing results of both treatments from a single institution.Study Design:Retrospective review.Methods:Review was made of 25 patients undergoing gentamicin injection and 39 patients undergoing vestibular nerve section for Meniere's disease. Rate of vertigo control and pretreatment and post‐treatment pure‐tone average values and speech discrimination scores were reported.Results:The mean preoperative pure‐tone average for patients having vestibular nerve section was 47.2 dB, with a speech discrimination score of 75.4%. In these patients, the postoperative pure‐tone average was 49.1 dB and the speech discrimination score was 75%. Patients undergoing gentamicin injection had a mean pretreatment pure‐tone average of 55.9 dB and a speech discrimination score of 62%. The post‐treatment pure‐tone average and speech discrimination score for the gentamicin group were 68.8 dB and 49.3%, respectively. Five of 25 patients (20%) in the gentamicin treatment group and 1 of 39 (3%) in the vestibular nerve section treatment group had an increase in bone‐conduction threshold greater than 30 dB. The amount of postprocedure hearing loss was significantly greater in the gentamicin treatment group (P = .006). Control of vertigo was good to excellent in 95% of the patients treated with vestibular nerve section and in 80% of the patients treated with gentamicin.Conclusion:Although vestibular nerve section and transtympanic gentamicin are both acceptable treatment options for vertigo associated with Meniere's disease, gentamicin causes a higher level of hearing loss related to treatment and vestibular nerve section has higher vertigo control rates.