A tissue-selective prostaglandin E2 analog with potent antifertility effects

Summary N-methanesulfonyl 16-phenoxy--tetranor PGE₂ is a prostaglandin analog which is markedly more tissue selective than PGE₂. This compound is 10–30 times more potent than PGE₂ in animal models which are considered relevant to antifertility effects in humans. In pharmacological tests which are believed to be predictive for side effects in humans, the compound has potency either equal to or less than that of PGE₂.     

Permeation of purine derivatives into the cerebrospinal fluid of dogs

Zusammenfassung Der Übertritt verschiedener Purinderivate in den Liquor cerebrospinalis nach i.v. Injektion wurde an Hunden untersucht. Coffein permeiert sehr schnell, Theobromin und Theophyllin ungleich langsamer. Dies steht in Einklang mit der unterschiedlichen Lipoidlöslichkeit dieser Substanzen. AAT hingegen tritt nur in geringer Konzentration in den Liquor über, obwohl es die höchste Lipoidlöslichkeit aufweist.     

Pharmacological studies with some new antihypertensive aminoquinazolines

Zusammenfassung 4 neue Aminoquinazolin-Derivate, die den Blutdruck von Hunden und Katzen herabsetzen, werden beschrieben. Ihre wirksamen Dosen liegen im Bereiche von 20 bis 300µg/kg peroral. Diese Substanzen setzen den peripheren Widerstand herab und reduzieren die blutdrucksteigernde Wirkung von Adrenalin, unterscheiden sich aber von den typischen-Sympatholytika.     

LDL-receptor-related proteins in Wnt signal transduction

The Wnt family of secreted signalling molecules are essential in embryo development and tumour formation. The Frizzled (Fz) family of serpentine receptors function as Wnt receptors, but how Fz proteins transduce signalling is not understood. In Drosophila, arrow phenocopies the wingless (DWnt-1) phenotype, and encodes a transmembrane protein that is homologous to two members of the mammalian low-density lipoprotein receptor (LDLR)-related protein (LRP) family, LRP5 and LRP6 (refs 12-15). Here we report that LRP6 functions as a co-receptor for Wnt signal transduction. In Xenopus embryos, LRP6 activated Wnt-Fz signalling, and induced Wnt responsive genes, dorsal axis duplication and neural crest formation. An LRP6 mutant lacking the carboxyl intracellular domain blocked signalling by Wnt or Wnt-Fz, but not by Dishevelled or beta-catenin, and inhibited neural crest development. The extracellular domain of LRP6 bound Wnt-1 and associated with Fz in a Wnt-dependent manner. Our results indicate that LRP6 may be a component of the Wnt receptor complex.     

A novel type of cardiac calcium channel in ventricular cells

Calcium influx is vital for several aspects of cardiac activity, so it is important to ask if heart cells possess a single or multiple types of Ca channel. Only one Ca channel type has been identified in patch-clamp studies of unitary current, despite suggestions to the contrary from whole-cell recordings in heart cells and unitary recordings from other cells. Here we describe a novel type of cardiac Ca channel with several properties that distinguish it from the hitherto-identified Ca channel in heart cells. Its conductance in isotonic Ba is small (8 pS), and is no larger in Ba than in Ca. It activates and inactivates at relatively negative potentials and remains functional long after patch excision. It is insensitive to dihydropyridines such as nimodipine and the Ca agonist Bay K 8644, and is more resistant to block by external Cd than the previously described type of cardiac Ca channel.     

Elemental compartmentalization in seeds of Atriplex triangularis and Atriplex confertifolia

Seeds of two halophytes, Atriplex triangularis, which grows in a mesic saline marsh environment, and Atriplex confertifolia, which grows in a xeric desert environment, were analyzed by energy-dispersive X-ray microanalysis for the distribution of elements. The highest concentration of sodium, chlorine, potassium, and calcium was present in seed coats of A. triangularis. All of the elements detected were at low concentrations in the endosperm. Embryos contained the highest amount of phosphorus that is probably associated with organophosphate compounds. Potassium was also high in embryos. The total amount of elements in all regions of A. confertifolia was low as compared to A. triangularis. In a similar pattern sodium, chlorine, potassium, and calcium were the highest in seed coats of A. confertifolia. Elemental concentration was also low in the endosperm. Likewise, the phosphorus level was the highest in the embryo. The results support the concept of elemental compartmentalization in seeds of these halophytes.     

Computer analysis of cross sections of leaves of Chrysothamnus taxa and their relation to environmental conditions

Thirty-eight accessions of 20 taxa (species and subspecies) of Chrysothamnus from a range of environments were grown in a uniform garden. During mid-June, terminal and lateral leaves were removed, fixed, and processed for light-microscopy studies. Area and perimeter measurements of ink tracings of midleaf vein cross sections were measured using computer-scan techniques. Leaf area and perimeter were compared with vein perimeter and area measurements. Area and perimeter of these Chrysothamnus leaves varied in response to the environment at the collection location. Plants native to hot, dry conditions had small, thick leaves, whereas plants native to cooler, more mesic conditions had relatively large, thin leaves. Similarly, leaves with round veins were adapted to hot, dry environments and leaves with elliptical veins were adapted to cooler, more mesic environments. Both terminal (young) and lateral (older) leaves were sampled. Terminal leaves showed significant (p < .05) correlational responses to environmental parameters, whereas the lateral leaves, while fronding in the predicted morphological directions, did not generally show significant responses. The different responses of terminal and lateral leaves may have been due to canopy position and uniform environmental conditions of the garden. Leaves with large cross sections characteristically had large veins, and leaves with small cross sections characteristically had small veins. Large leaf cross sections were normally flat. Small leaf cross sections were normally round. Decreasing leaf size and increasing leaf thickness were correlated with aridity.     

Preliminary observations of a bacteriophage infectingXenorhabdus luminescens (Enterobacteriaceae)

A bacteriophage infective toXenorhabdus luminescens, a bacterial symbiont of heterorhabditid nematodes, was recovered from insects that supported poor nematode development. Plaque tests showed the phage particles to be infective only to primary and not secondary colonies ofX. luminescens. The phage was not infective toX. nenatophilus primaries or secondaries. The bacteriophage particles ranged 80–90 nm in length, with the head ranging from 40 to 50 nm in diameter. Restriction analysis was performed on isolated bacteriophage DNA. This first report of a bacteriophage fromXenorhabdus species has pratical implications since it could be detrimental to cultures ofHeterorhabditis nematodes that are being produced throughout the world for the biological control of insects.