Design, Synthesis and SAR Analysis of Novel Potent and Selective Small Molecule Antagonists of NPBWR1 (GPR7).
Design, synthesis and SAR analysis of novel potent and selective small molecule antagonists of NPBWR1 (GPR7).
Filed under: Eating Disorders
Bioorg Med Chem Lett. 2012 Oct 2;
Urbano M, Guerrero M, Zhao J, Velaparthi S, Adrian Saldanha S, Chase P, Wang Z, Civelli O, Hodder P, Schaeffer MT, Brown S, Rosen H, Roberts E
Novel small molecule antagonists of NPBWR1 (GPR7) are herein reported. A high-throughput screening (HTS) of the Molecular Libraries-Small Molecule Repository library identified 5-chloro-4-(4-methoxyphenoxy)-2-(p-tolyl)pyridazin-3(2H)-one as a NPBWR1 hit antagonist with micromolar activity. Design, synthesis and structure-activity relationships study of the HTS-derived hit led to the identification of 5-chloro-2-(3,5-dimethylphenyl)-4-(4-methoxyphenoxy)pyridazin-3(2H)-one lead molecule with submicromolar antagonist activity at the target receptor and high selectivity against a panel of therapeutically relevant off-target proteins. This lead molecule may provide a pharmacological tool to clarify the molecular basis of the in vivo physiological function and therapeutic utility of NPBWR1 in diverse disease areas including inflammatory pain and eating disorders.
HubMed – eating
Nutrition-labeling regulation impacts on restaurant environments.
Filed under: Eating Disorders
Am J Prev Med. 2012 Nov; 43(5): 505-11
Saelens BE, Chan NL, Krieger J, Nelson Y, Boles M, Colburn TA, Glanz K, Ta ML, Bruemmer B
Recent attempts to improve the healthfulness of away-from-home eating include regulations requiring restaurants to post nutrition information. The impact of such regulations on restaurant environments is unknown.To examine changes in restaurant environments from before to after nutrition-labeling regulation in a newly regulated county versus a nonregulated county.Using the Nutrition Environment Measures Survey-Restaurant version audit, environments within the same quick-service chain restaurants were evaluated in King County (regulated) before and 6 and 18 months after regulation enforcement and in Multnomah County (nonregulated) restaurants over a 6-month period. Data were collected in 2008-2010 and analyses conducted in 2011.Overall availability of healthy options and facilitation of healthy eating did not increase differentially in King County versus Multnomah County restaurants aside from the substantial increase in onsite nutrition information posting in King County restaurants required by the new regulation. Barriers to healthful eating decreased in King County relative to Multnomah County restaurants, particularly in food-oriented establishments. King County restaurants demonstrated modest increases in signage that promotes healthy eating, although the frequency of such promotion remained low, and the availability of reduced portions decreased in these restaurants. The healthfulness of children’s menus improved modestly over time, but not differentially by county.A restaurant nutrition-labeling regulation was accompanied by some, but not uniform, improvements in other aspects of restaurant environments in the regulated compared to the nonregulated county. Additional opportunities exist for improving the healthfulness of away-from-home eating beyond menu labeling.
HubMed – eating
Energy intake from restaurants: demographics and socioeconomics, 2003-2008.
Filed under: Eating Disorders
Am J Prev Med. 2012 Nov; 43(5): 498-504
Powell LM, Nguyen BT, Han E
Eating food away from home and restaurant consumption have increased over the past few decades.To examine recent changes in calories from fast-food and full-service restaurant consumption and to assess characteristics associated with consumption.Analyses of 24-hour dietary recalls from children, adolescents, and adults using nationally representative data from the 2003-2004 through 2007-2008 National Health and Nutrition Examination Surveys, including analysis by gender, ethnicity, income, and location of consumption. Multivariate regression analyses of associations between demographic and socioeconomic characteristics and consumption prevalence and average daily caloric intake from fast-food and full-service restaurants.In 2007-2008, 33%, 41%, and 36% of children, adolescents, and adults, respectively, consumed foods and/or beverages from fast-food restaurant sources and 12%, 18%, and 27% consumed from full-service restaurants. Their respective mean daily caloric intake from fast food was 191, 404, and 315 kcal, down by 25% (p?0.05), 3%, and 9% from 2003-2004; and among consumers, intake was 576, 988, and 877 kcal, respectively, down by 12% (p?0.05), 2%, and 7%. There were no changes in daily calories consumed from full-service restaurants. Consumption prevalence and average daily caloric intake from fast-food (adults only) and full-service restaurants (all age groups) were higher when consumed away from home versus at home. There were some demographic and socioeconomic associations with the likelihood of fast-food consumption, but characteristics generally were not associated with the extent of caloric intake among those who consumed from fast-food or from full-service restaurants.In 2007-2008, fast-food and full-service restaurant consumption remained prevalent and a source of substantial energy intake.
HubMed – eating
Does olfactory specific satiety take place in a natural setting?
Filed under: Eating Disorders
Appetite. 2012 Oct 15;
Fernandez P, Bensafi M, Rouby C, Giboreau A
Olfactory-specific satiety (OSS) is characterized by a specific decrease in the odor pleasantness of a food eaten to satiety or smelled without ingestion. The usual protocol for studying OSS takes place in laboratory, a setting rather removed from the real world. Here, we set out to examine OSS in a natural setting: during a meal in a restaurant. We hypothesized that an aroma contained in a food that is eaten at the beginning of a meal decreases the pleasantness of the flavor of a food with the same aroma eaten at the end of the meal. In the first experiment (Experiment 1), a test group received an appetizer flavored with a test aroma (anise) at the beginning of the meal. After the main dish, they received a dessert flavored with the same aroma. A control group received the same aromatized dessert, but after a non-aromatized appetizer. This experiment was replicated (Experiment 2) using verbena as the test aroma. For both experiments, results revealed that aroma pleasantness, but not intensity or familiarity, significantly decreased in the test groups vs. the control groups. These findings extend the concept of OSS to a realistic eating context.
HubMed – eating
Assessing eating context and fruit and vegetable consumption in children: new methods using food diaries in the UK national diet and nutrition survey rolling programme.
Filed under: Eating Disorders
Int J Behav Nutr Phys Act. 2012 Oct 18; 9(1): 126
Mak TN, Prynne CJ, Cole D, Fitt E, Roberts C, Bates B, Stephen A
ABSTRACT: BACKGROUND: Eating context is the immediate environment of each eating occasion (EO). There is limited knowledge on the effects of the eating context on food consumption in children, due to the difficulty in measuring the multiple eating contexts children experience throughout the day. This study applied ecological momentary assessment using food diaries to explore the relationships between eating context and fruit and vegetable consumption in UK children. METHODS: Using 4 d unweighed food diaries, data were collected for 642 children aged 1.5-10y in two years of the UK National Diet and Nutrition Survey (2008–2010). Participants recorded all foods and drinks consumed at each EO, where and with whom the food was consumed, whether the TV was on and if eaten at a table. Mixed logistic regression and mixed multinomial logistic regression were used to calculate associations between eating contexts and fruit and vegetables (FV) consumed by quartiles. RESULTS: Of 16,840 EOs, 73% took place at home and 31% with parents only. Frequency of eating alone and with friends increased with age. Compared to eating at home, children aged 1.5-3y were more likely to consume fruit at care outside home (>10-50g OR:2.39; >50-100g OR:2.12); children aged 4-6y were more likely to consume fruit (>50-100g OR:3.53; >100g OR:1.88) and vegetables at school (>30-60g OR:3.56). Compared to eating with parents only, children aged 1.5-3y were more likely to consume fruit with friends (>10-50g OR:2.69; >50-100g OR:3.49), and with carer and other children/others (>10-50g OR:2.25); children aged 4-6y were more likely to consume fruit (>50-100g OR:1.96) and vegetables with friends (>30-60g OR:3.56). Children of all ages were more likely to eat vegetables when the TV was off than on and at a table than not at table. CONCLUSIONS: The use of food diaries to capture multiple eating contexts and detailed fruit and vegetable consumption data was demonstrated at a population level. Higher odds of FV consumption were seen from structured settings such as school and care outside home than at home, as well as when eating at a table and the TV off. This study highlights eating contexts where provision of fruit and vegetables could be improved, especially at home. Future research should take eating context into consideration when planning interventions to target children’s food consumption and eating behaviour.
HubMed – eating
Eating Disorders: When Food Hurts Part 1/2 – Eating Disorders: When Food Hurts
More Eating Disorders Information…