Identification of Psychoplastogenic Tropanes Lacking Muscarinic Activity.

Tropane-containing small molecules like scopolamine are a promising class of psychoplastogens. However, their potent antagonism of all muscarinic receptor subtypes presents the potential for undesirable anticholinergic side effects. In an effort to decouple their neuroplasticity-promoting effects from their muscarinic activity, we performed phenotypic structure-activity relationship studies across a variety of structurally distinct subclasses of tropanes.

Rapid Synthesis of Psychoplastogenic Tropane Alkaloids.

Tropane alkaloids are an important class of biologically active small molecules characterized by their 8-azabicyclo[3.2.1]octane core.

5-HT2ARs Mediate Therapeutic Behavioral Effects of Psychedelic Tryptamines.

Psychedelic compounds have displayed antidepressant potential in both humans and rodents. Despite their promise, psychedelics can induce undesired effects that pose safety concerns and limit their clinical scalability. The rational development of optimized psychedelic-related medicines will require a full mechanistic understanding of how these molecules produce therapeutic effects.

Forest structure and composition alleviate human thermal stress.

Current climate change aggravates human health hazards posed by heat stress. Forests can locally mitigate this by acting as strong thermal buffers, yet potential mediation by forest ecological characteristics remains underexplored. We report over 14 months of hourly microclimate data from 131 forest plots across four European countries and compare these to open-field controls using physiologically equivalent temperature (PET) to reflect human thermal perception.

Synthesis of Tertiary Amines through Extrusive Alkylation of Carbamates.

Basic amines are key elements of many biologically active natural products and pharmaceuticals. Given their inherent reactivity, it is often necessary to protect basic amines during target-directed synthesis, which results in wasteful protection/deprotection sequences. We report a step-economical approach enabling the protection of secondary amines as carbamates prior to their conversion to tertiary amines via the formal extrusion of CO.

How 'hot' is too hot? Evaluating acceptable outdoor thermal comfort ranges in an equatorial urban park.

Urban green spaces offer vital ecosystem services such as regulating elevated temperatures in cities. Less information exists, however, on how urban green spaces influence outdoor thermal comfort (OTC), which is dependent on people's perceptions of the complex interactions amongst ambient humidity, wind and both air and radiant temperatures. In this study, we analysed an existing OTC dataset compiled within a large Singapore urban park and calibrated OTC thresholds for physiological equivalent temperatures (PET) by analysing PET against thermal perception survey responses from the park visitors (n = 1508).

Patterns of land change and their potential impacts on land surface temperature change in Yangon, Myanmar.

This study used remote sensing imagery to characterize land use/cover patterns and to derive land surface temperature (LST) of Greater Yangon, the largest urban agglomeration in Myanmar, to provide insights into the association between land use/cover and seasonal, daytime, and nighttime LST change. Analysis of Landsat images from 1987 to 2015 showed urban expansion radiating from the city center and along prominent rivers, with major increases in built-up land (6.4%) and grassland (10.

Long-term safety and clinical effectiveness of controlled-release metoclopramide in cancer-associated dyspepsia syndrome: a multicentre evaluation.

Patients with cancer frequently report gastrointestinal symptoms such as anorexia, early satiety, nausea, vomiting, and bloating. A reduction of the severity of some of these symptoms would benefit the patient by enhancing quality of life and improving their treatment. Forty-eight patients (25 female and 23 male; mean age 63 +/- 11 years) with a minimum two-week history of cancer-associated gastrointestinal symptoms were assigned to a single, open-label treatment group and received controlled-release metoclopramide 20 mg-80 mg q12h for a maximum period of 12 weeks (mean 46 +/- 35 days).