On the urinary elimination of methoxypromazine in man

Zusammenfassung Die Ausscheidung eines neuen neuroleptisch wirksamen Phenothiazinderivates — Mopazin — im Harn wurde spektrophotometrisch und papierchromatographisch untersucht. Als wichtigstes Abbauprodukt wurde Methoxypromazin-sulfoxyd gefunden. Daneben waren unverändertes Methoxypromazin und 1–3 nicht identifizierte Abbauprodukte nachzuweisen. Bei den letzteren handelt es sich möglicherweise um Konjugate.     

Effect of choline salicylates and some other analogues of salicylic acid on the replication of EMC virus in vitro

Zusammenfassung Es wird eine 90–99,9%ige Hemmung in vitro der Replikation des EMC-Virus durch 0,5–2 m molare Lösungen folgender Salicylsäurederivate festgestellt: Cholinsalicylat, Cholinacetoxysalicylat und der Natriumsalze von 2-Merkaptobenzoesäure, Salicylsäure sowie Acetylsalicylsäure. Ferner wurde eine etwa 70%ige Hemmung des Natriumsalzes der Sulphosalicylsäure, des Cholin-p-chlorobenzoates, sowie des Cholin-o-chlorobenzoates beobachtet. Cholin-p-oxybenzoat und Cholin-p-acetoxybenzoat zeigten hingegen keine Hemmungsaktivität.

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Acknowledgements: We are indebted to Drs. Z.Macho and T.Zawisza from the Department of Synthesis of Drugs, School of Medicine, Wroclaw, for donating of choline salicylates and other derivatives of benzoyl-choline⁶.     

Sexual dimorphism in contraction properties and fibre of the flexor carpi radialis muscle of the frog (Rana temporaria L.)

Zusammenfassung Es wird ein Sexualdimorphismus beim Daumenbeugemuskel (m. flexor carpi radialis) des Frosches (Rana temporaria L.) mit Bezug auf das Kontraktionsverhalten, wie auch in histochemischer Richtung, festgestellt. Kontraktions- und Relaxationszeit sind bei männlichen Muskeln veralaugsamt mit entsprechender ATPase-Aktivität. Saionbedingte, geschlechtstypische Testosteronkonzentrationen stehen damit im Zusammenhang.     

Non-steroidal anti-inflammatory drugs: Effects on the utilization of glucose and production of lactic acid in tissue culture

Zusammenfassung In der Kultur embryonalen Hühnchengewebes kommt es unter Einfluss nichtsteroider Antiphlogistica (Aspirin, Indomethacin, Mefenamicsäure) zu einer Steigerung des Glukoseverbrauchs bei gleichzeitiger Vermehrung der Milchsäureerzeugung. Der Milchsäureverbrauch verläuft in zwei Phasen, wobei der erste Gipfel bei geringsten Konzentrationen des Arzneimittels.auftritt.     

Serotonin inhibition of liver mitochondria swellingin vitro

Riassunto È stato studiato l'effetto della serotonina sul rigonfiamento dei mitocondriin vitro: si è trovato che la serotonina protegge i mitocondri dal rigonfiamento spontaneo che si ha quando vengono sospesi in soluzione isotonica di saccarosio.     

Open channel structure of MscL and the gating mechanism of mechanosensitive channels

Mechanosensitive channels act as membrane-embedded mechano-electrical switches, opening a large water-filled pore in response to lipid bilayer deformations. This process is critical to the response of living organisms to direct physical stimulation, such as in touch, hearing and osmoregulation. Here, we have determined the structural rearrangements that underlie these events in the large prokaryotic mechanosensitive channel (MscL) using electron paramagnetic resonance spectroscopy and site-directed spin labelling. MscL was trapped in both the open and in an intermediate closed state by modulating bilayer morphology. Transition to the intermediate state is characterized by small movements in the first transmembrane helix (TM1). Subsequent transitions to the open state are accompanied by massive rearrangements in both TM1 and TM2, as shown by large increases in probe dynamics, solvent accessibility and the elimination of all intersubunit spin-spin interactions. The open state is highly dynamic, supporting a water-filled pore of at least 25 A, lined mostly by TM1. These structures suggest a plausible molecular mechanism of gating in mechanosensitive channels.     

Targeted mutation of Cyln2 in the Williams syndrome critical region links CLIP-115 haploinsufficiency to neurodevelopmental abnormalities in mice

Williams syndrome is a neurodevelopmental disorder caused by the hemizygous deletion of 1.6 Mb on human chromosome 7q11.23. This region comprises the gene CYLN2, encoding CLIP-115, a microtubule-binding protein of 115 kD. Using a gene-targeting approach, we provide evidence that mice with haploinsufficiency for Cyln2 have features reminiscent of Williams syndrome, including mild growth deficiency, brain abnormalities, hippocampal dysfunction and particular deficits in motor coordination. Absence of CLIP-115 also leads to increased levels of CLIP-170 (a closely related cytoplasmic linker protein) and dynactin at the tips of growing microtubules. This protein redistribution may affect dynein motor regulation and, together with the loss of CLIP-115-specific functions, underlie neurological alterations in Williams syndrome.     

Occurrence, persistence, and expansion of saltcedar ( Tamarix spp.) populations in the Great Plains of Montana

Saltcedar ( Tamarix spp.), a shrub native to Eurasia, is associated with major alterations to wetland and riparian systems in the southwestern United States. Since the 1960s saltcedar has been naturalized in northern states of the U.S. where its growth potential and impacts are not well known. Here, we describe the occurrence, age, size, and relative cover of saltcedar populations in several river basins in central eastern Montana, USA, to identify potential patterns of spread across the region and changes in individual populations as they age. Stands were aged according to the oldest saltcedar individuals and were sampled for dominant plant cover and soil properties. Multiple introductions appear to have occurred in Montana, with the oldest stands occurring on the Bighorn River in southern Montana. Saltcedar absolute and relative cover and stand area increased significantly with stand age, while native tree and shrub relative cover remained low across all stand ages. These results suggest that saltcedar stands establish where woody natives are not abundant and that they persist and expand over time. Although soil salinity remained constant, soil pH decreased with saltcedar stand age, indicating a possible effect of organic matter inputs. An analysis of annual wood increment of saltcedar and sandbar willow (a native with analogous growth form) stems along a latitudinal gradient showed that stem growth of both species did not differ significantly among regions. Stem growth decreased inversely with elevation for both species while growth responses to elevation did not differ between species. Our results show an increase in number of populations and continued viability of these populations. Mechanisms of saltcedar increases in this region are yet to be determined. Anthropogenic influences, such as saltcedar plantings, watershed alterations (e.g., river flow control), and habitat disturbances (e.g., cattle grazing or habitat clearing) may facilitate its spread in similar climates of the Great Plains.