Coenzymes Q: Stimulants of the phaǵocytic activity in rats and immune response in mice

Zusammenfassung Mittels der Tusche-Clearance-Methode wird gezeigt, dass Coenzym Q₆ und Q₁₀ die phagozytische Aktivität bei Ratten steigert. Im Vergleich mit Schaferythrozyten wurde bei Mäusen durch Zufuhr von Coenzym Q₁₀ eine Verdoppelung der primären hämolytischen Antikörperbildung festgestellt.

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The authors are deeply indebted to Drs. J. H.Heller, J. H.Green and A. D.Adler for support and helpful discussions in the course of this work. We thank Mrs. G.Katopodis, Mrs. R.Wells, Miss J.Mannion, Mrs. S._Reynolds and Mrs. A._Lee for technical assistance.     

Effect of various solubilizers on angiotensinII receptors in bovine adrenocortical plasma membranes

Summary 3 monionic detergents, Triton X-100, Lubrol WX and NP-40, inhibited binding of [³H]-AT_II to bovine adrenocortical plasma membranes. This effect appeared to be direct and not due to solubilization of the AT_II receptor by these agents. Sodium deoxycholate and the chaotropic ions, ClO ₄ ^– and Br^–, produced effects similar to the nonionic detergents.Supported by grants from the Quebec Heart Foundation and the Medical Research Council of Canada. The authors acknowledge the technical assistance of Mrs D. Michaud and the secretarial aide of Mrs D. Huot-Blais, and Miss L. Leblanc.     

The number of parallel fibre-Purkinje dendrite synapses. A morphometric evaluation

Summary Quantitative parameters concerning synapses were studied in the cerebellar molecular layer of 4 cats using ultrastructural morphometric methods. The number of parallel fibre-Purkinje dendrite synapses was estimated to be about 200,000.This study was granted by I.N.I.C. (Centro de Morfologia Experimental—MbP₁ e Centro de Anatomia Patológica e Oncologia-MbP₃).The authors thank Mrs M.L. Brito, Mrs M.A. Nascimento, Mrs M.G. Rodrigues and Mr L.B. Nunes for their technical assistance.     

Effect of halogenmethylenebisphosphonates on bone cells in culture and on bone resorption in vivo

Summary Dihalogenmethylenebisphosphonates increase alkaline phosphatase activity and fatty acid oxidation in calvaria cells in culture (Cl₂MBP>Br₂MBPF₂MBP). The monohalogen C1MBP and the non-halogenated analogues are less active on phosphatase and inactive on or inhibitory towards fatty acid oxidation. The three dihalogenbisphosphonates and C1MBP inhibit bone resorption in vivo, Cl₂MBP most strongly.Acknowledgments. We thank Miss M.-L. Aebersold, Miss J. Portenier, Mrs I. Tschudi and Mrs Ch. Marti for their skilled technical assistance. This work has been supported by the Swiss National Science Foundation (grant 3.937.82), by the Procter & Gamble Company, Cincinnati, USA, by the Istituto Gentili S.p.A., Pisa, Italy, and by the Ausbildungs- und Förderungsfonds der Arbeitsgemeinschaft für Osteosynthese (AO), Chur, Switzerland.     

In vitro inactivation of corpora allata of the bugOncopeltus fasciatus by precocene II

Summary Corpora allata fromOncopeltus fasciatus incubated in vitro in medium containing 10^–5.35 M (1 g/ml) of precocene II lose their ability to secrete juvenile hormone when reimplanted into last instar larvae.Acknowledgments. We thank Mr K. Dorn, Mrs L. Dolezal, Mrs V. Nötzli-Graf, Mr K.H. Trautmann and Mr A. Schuler for technical help, Dr W. Vogel and Dr A. Dübendorfer for valuable discussions.     

Inhibitory effects of 1-iodo-3-aminomethyl-5,6,7,8-tetrahydro-2-naphthol (ONO-3122) and prostaglandin H2 on vasopressin-induced osmotic water flow in toad bladder

Summary Both 1-iodo-3-aminomethyl-5,6,7,8-tetrahydro-2-naphthol (ONO-3122), which increases endogenous PGH₂, and PGH₂ itself, significantly depressed vasopressin-induced osmotic water flow in the toad bladder. These results suggest that ONO-3122 increases endogenous PGH₂ synthesis, and that PGH₂ and/or its metabolites inhibit vasopressin-induced water flow.I am grateful to Mr Y. Nara and Mrs S. Sugawara for their excellent technical assistance. This work supported in part by grant from the Life Science Laboratories.     

Interaction of platinum compounds with bacterial DNA

Summary The cis and trans isomer of PtCl₂(NH₃)₂, cis-Pt(cpa)₂Cl₂ and 2 platinum pyrimidine blues have been used in a number of bacterial tests indicative of their interaction with bacterial DNA.This investigation was supported by a grant from C.N.R., Rome. We thank Mrs S. Saincich for skilful technical assistance.     

Effects of anaesthesia and chronic catheterization on circulating levels of prostaglandins (PGE2 and PGF2a in dogs

Summary Chronic catheterization of aorta and inferior vena cava in dogs did not significantly affect circulating levels of prostaglandins (PGE₂ and PGF_2a ). Pentobarbital (30 mg/kg i.v.) anaesthesia produced a significant decrease in PGF_2a .This work was supported by INSERM (grant No. 76.5.183.5).We wish to thank Miss Laure Eloy and Mrs Annick Soubrier for their technical assistance.     

Potentiation of ocular response to adrenaline by 3,3-dimethyl-1-[3-methylaminopropyl]-1-phenylphthalan (Lu 3-010) and a thiophthalan analogue (Lu 5-003): Blockers of catecholamine uptake

Résumé Concernant la durée de l'effet du traitement, le composé Lu 3-010 en combinaison avec l'adrenaline est semblable à la protriptyline, et il est plus actif que Lu 5-003 en ce qui concerne la potentiation de la reaction oculaire provoquée par l'adrenaline. Administrés séparement, les composés Lu 3-010 et Lu 5-003 ont des effets semblables, tandis que la protriptyline est le composé le plus actif. L'accroissement de l'efficacité de ces composés résulte probablement de leur abilité à bloquer le mécanisme de l'incorporation de la catecholamine.

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The author acknowledges the technical assistance of Mrs.S. Schaal, Mrs.C. Wood, MissB. Kawchak and Mrs.B. Sumner. The Lu compounds were gifts from H. Lundbeck and Co. Ltd.     

A new type of ‘node’ in the myelin sheath of an invertebrate nerve fibre

Zusammenfassung Es werden neuartige, segmental angeordnete Öffnungen in der Myelinscheide der medianen Riesenfaser des RegenwurmsLumbricus terrestris beschrieben, durch welche die Axonmembran direkt an die extrazelluläre Kollagenhülle des Bauchmarkperineuriums heranreicht. Dieser Befund wird in Hinblick auf den Mechanismus der Erregungsleitung myelinisierter Nervenfasern von Wirbellosen diskutiert.

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This work was suported in part by a DFG Grant No. Gu/117/1. The technical assistance of Mrs.H. Eggert is thankfully acknowledged.     

Effect of harmaline on the cerebello-rubral system

Summary Harmaline induces synchronous rhythms in both the cerebellum and the red nucleus of the rabbit. The level of synchronization is lower in the red nucleus than in the cerebellar cortex, probably because the cerebello-rubral pathway and the red nucleus neurons only participate poorly in the harmaline-induced olivo-cerebellar rhythm.Acknowledgments. We thank Mrs M. Satzinger and Mrs A. Motejlek for their technical assistance. The drugs were generously supplied by Bayer Pharma GmbH, Vienna (Evipan^® and Epontol^®), Boehringer, C. H. Sohn, Ingelheim am Rhein, Federal Republic of Germany (Flaxedil^®) and Hoffmann-La Roche GmbH, Vienna (harmaline hydrochloride).     

Effect of des-Tyr1-γ-endorphin on serotonin metabolism in rat brain regions

Summary Intracerebroventicular (i.c.v.) administration of des-Tyr¹-γ-endorphin (0.1 and 1.0 μg) caused a decrease of the serotonin (5-HT) concentration of the hippocampus. The concentration of 5-HIAA and the pargyline-induced alterations in 5-HT and 5-HIAA were not affected. No effects were noticed in other brain regions. Acknowledgement. The skilful technical assistance of Ms Henny de Vos Burchart-Lodewijks and Mrs H.A. Spierenburg and J.A. Meijer is gratefully acknowledged. Des-Tyr¹-γ-endorphin was a gift of Dr. H.M. Greven, Organon International B.V., Oss, The Netherlands. To whom reprint requests should be addressed.     

Cold stress induced changes in the uptake and distribution of radiolabelled magnesium in the brain and pituitary of the rat

Résumé L'imposition de conditions hypothermiques augmente l'incorporation de²⁸Mg dans le cerveau et la glande pituitaire du rat.

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Research for this paper was supported by NSF No. GB 27740 X. The authors are grateful for the technical assistance of Mrs.M. Turner, Mrs.E. Rovner and Mrs. L. Macko.     

Changes of the prostaglandin F23 metabolism in early human placenta

Summary The quantitative metabolism of PgF₂₄ was studied in different ages of early human placentae in vitro. The 15-OH-Pg-dehydrogenase became minimal at about the 9th week.This work was supported in part by WHO.The authors are indepted to Miss M. Pasztor, Mrs V. Palinkas and Miss G. Odrobina.     

5-Methylangelicin: A new highly photosensitizing angular furocoumarin

Summary 5-Methylangelicin, a new highly photosensitizing angular furocoumarin, was studied in 2 different biological systems, the T₂ phage and Ehrlich ascites tumor cells; in comparison with angelicin, the parent compound, it was several times more active.Acknowledgments. The authors wish to thank Mrs M. Peron for her excellent technical assistance.     

Synthesis,crystallization and properties of acetyl phenylalanyl lysine chloromethyl ketone: A potential inhibitor of serine proteases

Summary A procedure for the synthesis of acetyl phenylalanyl lysine chloromethyl ketone is described. The chloromethyl ketone derivative is a noncompetitive inhibitor of trypsin (K₁=5.9×10^–3 M).Acknowledgments. The authors are grateful to Dr Arthur L. Bacon for his constant support and encouragement. Special thanks are due to Dr William Kray for initiating this research project. We thank Mrs Juliette Barclay, Ms Earlene Spratling and Ms Ollivette Hill for their technical assistance in conducting some of the experiments. This investigation was supported by MBS grant RR8105 from the General Research Support Branch, Division of Research Resources, National Institutes of Health.     

The deamino derivatives of [4-threonine]-oxytocin and [4-threonine]-mesotocin; Analogs possessing a surprising spectrum of diminished pharmacological activities

Zusammenfassung Synthese (Merrifield-Methode) und pharmakologische Eigenschaften der Desamino-Derivate von (4-Threonin)-Oxytocin und (4-Threonin)-Mesoxytocin werden beschrieben.

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This work was supported in part by the Medical College of Ohio, a Contract (No. 69-2193) from the Center for Population Research of the National Institute of Child Health and Human Development, Research Grants from the National Science Foundation (No. GB-4932), the National Institute of Arthritis and Metabolic Diseases (No. AM-01940) and a General Research Support Grant to Columbia University from the National Institutes of Health. The authors wish to thank Mrs.Sara Crumm for performing the amino acid analyses and Mrs.Margot Acosta for performing the bioassays. An abstract of part of this work was presented at the 2nd American Peptide Symposium, Cleveland, Ohio, August 1970;M. Manning andW. H. Sawyer,Peptides (Ed.Saul Lande, Gordon and Breach, New York 1971), in press.     

Effect of 15(R)-15-methyl-prostaglandin E2 on iron absorption in the rat

Summary The administration of 15(R)-15-methyl prostaglandin E₂ (15(R)-15-M-PGE₂) in vivo significantly diminished the uptake of⁵⁹Fe into blood, spleen, liver, femur and dried intestine of rats, whereas acetylsalicylic acid (ASA) increased the counts significantly. This effect of ASA was counteracted by 15(R)-15-M-PGE₂. It is suggested that prostaglandins (PGs) might play an important role in inhibiting iron absorption at the intestinal level.This work was supported by grant No.6638 from CONICET (Argentina). The technical assistance of Mrs María E. Castro and Norma Rizzo is gratefully acknowleged.     

Enantiomeric cannabinoids: stereospecificity of psychotropic activity

Summary The 1,1-dimethylheptyl homolog of (–)-(3R,4R)-7-hydroxy-delta-6-tetrahydrocannabinol (compoundII) is highly psychotropic in mice, rats and pigeons. The (+)-(3S,4S) enantiomer (III) was found to be psychotropically inactive at doses up to several thousand times those of the ED₅₀ of (II).We thank Dr A. Breuer and Mrs H. Amsalem for help with the syntheses. The research reported above was supported in Tucson by NIH grant NS 15441; in Uppsala by grants from the Swedish Medical Research Council (5757) and the Swedish Council for the Planning and Coordination of Research (84/2082); in Jerusalem by the Szold Foundation.Presented in part at a meeting at the US National Institute on Drug Abuse, Washington, D.C., October 1986, see NIDA Research Monographs79 (1987) 15.