Structure-activity relationships of cyclic acetylcholine analogues of the piperidinol and thiacyclohexanol series.

The hydrochlorides and methiodides of 1-methyl-3- and 4-acetoxypiperidine and their sulphonium analogues are cholinergic agonists. They are substrates for acetylcholinesterase. The sulphonium compounds have a 78(-524)-fold higher activity than its nitrogen analogues.     

d-Aminosäurehaltige Analoga des Eledoisins

Summary The synthesis of several C-terminal eledoisin heptapeptide analogues, containing 1–5d-amino acids, is described and the biological activities are discussed.

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Über Peptidsynthesen XXXI. 4. Mitt. über Eledoisin und Eledoisin-Analoga. 3. Mitt. über Eledoisin und Eledoisin-Analoga:K. Lübke undE. Schröder, Liebigs Ann., im Druck.

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Auszugsweise vorgetragen auf dem VII. Europäischen Peptidsymposium, September 1964 in Budapest.     

Synthese und biologische Aktivität bradykininwirksamer Undeca-, Dodeca- und Tridecapeptide

Summary Several undeca-, dodeca- and tridecapeptides, analogues of the naturally occurring methionyllysyl-bradykinin, have been synthesized. The biological activities of the new compounds on the isolated rat uterus, guinea-pig ileum and rabbit blood pressure are presented.

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über Peptidsynthesen XXXIV. 7. Mitt. über Bradykinin- und Kallidin-Analoga. XXV. Mitt. über Peptidsynthesen, 6. Mitt. über Bradykinin- und Kallidin-Analoga:E. Schr?der, H.-S. Petras undE. Klieger, Liebigs Ann.679, 221 (1964).     

Über den Einfluss der Kettenlänge auf die biologische Aktivität eledoisinanaloger Verbindungen

Summary The syntheses of Eledoisin analogues by shortening the peptide chain at the N-terminal moiety of the molecule are described. The influence of the chain length on the hypotensive activity is discussed.

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Über Peptidsynthesen XXXII. 5. Mitt. über Eledoisin und Eledoisin-Analoga. 4. Mitt. sieheE. Schröder, K. Lübke undR. Hempel, Exper.21, 70 (1965).

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Auszugsweise vorgetragen auf dem 7. Europäischen Peptidsymposium in Budapest (Sept. 1964).     

Stabilität verschiedener Bradykininanaloga gegen kininase II

Summary Some analogues of bradykinin, especially with replacements by other amino acids of phenylalanine in position 8, have been investigated for enzymatic stability against kininase II from rat duodenum microsomes and rat uterus plasma membranes, respectively. As compared with bradykinin, two of the analogues, [8-erythro--phenylserine]-and [8-erythro--Amino--phenylbutyric acid]-Bradykinin were stable to enzymatic degradation. Therefore, the latter may be used for studies in hormone-receptor interaction.

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Mitteilung: Untersuchungen an bradykininbindenden Zellfraktionen.

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Frau Dr.M. P. Filatova aus dem Shemyakin-Institut für Bioorganische Chemie der Akademie der Wissenschaften der UdSSR, Moskau, danken wir für ihre Mitarbeit bei der Erstellung der Arbeitskonzeption. Für die Präparation der Membranen sei FrauT. Jankova, HerrnC. Liebmann und HerrnH. Steinmetzger herzlich gedankt. Wir danken Frl.R. Raspe, Frl.B. Schilling und FrauI. Agricola für die gute technische Mitarbeit bei der biologischen Wertbestimmung und der Präparation der Membran — bzw. Mikrosomenfraktion.     

Paradoxical inhibition of the effects of bradykinin by some sulfhydryl reagents

Résumé Plusieurs dérivés thiol et deux antioxidants inhibent la bronchoconstriction chez le cobaye, une partie de l'hypotension chez le lapin et la libération de «rabbit aorta contracting substance» (RCS) dues à la bradykinine Il est proposé que les effets communs à la bradykinine, à la SRS-A, SRS-C et à l'acide arachidonique, qui sont bloqués par des antiinflammatoires, acides, et par les dérivés thiol, sont dus à la formation de RCS, constituée par des péroxydes cicliques analogues aux précurseurs instables des prostaglandines E 2 et F 2 alpha.

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We thank MrsB. Charpentier andC. Bellevrat for technical help, Prof.H. Clauser andJ. R. Vane and DrH. O. J. Collier for comments and DrS. H. Ferreira for advice concerning the superfusion technique and for BPP9. Squibb provided BPP5. This work is part of a thesis leading to the degree of Docteur-ès-Sciences, Orsay (B.B.V.).     

Enhanced inhibition of RNA synthesis by amanitins in in vitro cultured cells

Summary The inhibition of RNA synthesis by -amanitin on vitro cultured cells is very slow. The action of various analogues of the toxin was tested and some of them proved more effective. Moreover pretreatment of cell cultures with DEAE-dextran greatly enhanced the effect of -amanitin.Acknowledgments. We thank ProfessorTh. Wieland and Dr.H. Faulstich (Max-Planck-Institut, Heidelberg) for the generous gift of amanitins. This investigation was supported by grant No. 74.00637.65 from C.N.R. (Roma).     

Immunoassay for lysine8-vasopressin (LVP): Comparison of biological and immunological activity of lysine-vasopressin and some of its synthetic analogues

Résumé Ces résultats suggèrent d'une part que¹²⁵I-LVP monoiodée a peu d'activité antidiurétique, d'autre part que le noyau phénylalanine en position 3 est essentiel pour la liaison de l'antigène à l'anticorps et que les sites immunologiques et biologiques de l'hormone sont différents.

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Acknowledgments. We wish to thank ProfessorS. Jard (Collège de France, 11, place Marcellin Berthelot, Paris 5^eme) for his valuable advice in connection with this work. LVP analogues were generously supplied by Dr.R. A. Boissonnas of Sandoz Pharmaceuticals.     

Geometrical constructions equivalent to non-linear algebraic transformations of the plane in Newton's early papers

Summary The theory of constructive formation of plane algebraic curves in Newton's writings is discussed in § 1: the apparatus by which Newton forms the curves, Newton's theorems on forming unicursal curves, his theory of conics, and his theory of (m, n) correspondence. Special Cremona plane and space transformations obtained by Newton's organic method are dealt with in § 2. The article ends with § 3, which shows two different directions in the theory of the constructive formation of plane algebraic curves in the XVIII-XIXth centuries. A synopsis is appended.Abbreviations MPN The Mathematical Papers of Isaac Newton, edited by D. T. Whiteside, Vols. 1–3, Cambridge, 1967–1969 - Hudson H. Hudson, Cremona Transformations in Plane and Space, Cambridge, 1927 - PT (abridged) Philosophical Transactions of the Royal Society 1665–1800 (abridged), London, 1809 - Andreev ₁ K. A. Andreev, On geometrical correspondences ... (in Russian), Moscow, 1879 - Andreev ₂ K. A. Andreev, On the Geometrical Formation of Plane Curves (in Russian), Kharkov, 1875     

Demonstration of a negative binding effect of bovine growth hormone toward potassium

Zusammenfassung Hochgereinigtes Rinderwachstumshormon besitzt ein ziemlich gutes Bindungsvermögen für Mg⁺⁺-, Ca⁺⁺- und Na⁺-Ionen. Andererseits wird K⁺ je nach Konzentration überhaupt nicht, oder nur in Spuren gebunden.

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The performance of the elementary analyses by R. C.Anderson is gratefully acknowledged. Thanks are also due to B.Czuk and N. O.Milkovich for technical assistance.     

Synthesis of L-4-amino-3-isoxazolidinone,the unnatural stereoisomer of cycloserine and its antibiotic activity

Zusammenfassung Eine direkte Synthese vonl- undd-Cycloserin ausl- undd-Serin wurde beschrieben. Die bakteriostatischen Effekte der drei Formen von Cycloserin (d-,l-unddl-) aufE. coli in synthetischem Medium wurden verglichen.     

Evoked release of 5-HT and NEFA from the hypothalamus of the conscious monkey during thermorégulation

Zusammenfassung Unterkühlungsexperimente mit Affen zeigen einen Anstieg des 5-HT-Gehaltes in der Durchströmungsflüssigkeit des vorderen Hypothalamus. Erwärmung der Tiere ergab 2–4fachen Anstieg eines NEFA-ähnlichen Stoffes.

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Supported in part by U.S. Office of Naval Research Contract No. N00014-67-A-0226-0003, Grant No. GB 7906 from the National Science Foundation and a grant from the Wallace Laboratories. The authors are indebted to P.Cuezon, J. E.Evans and R. B.Holman for their valuable assistance.     

Ultrastructural identification of human tonsil T-lymphocytes by peroxidase-conjugated anti-HTLA serum

Summary A horse anti-serum rendered specific for human T-lymphocytes was conjugated with peroxidase and used for ultrastructural identification of human tonsil T-lymhocytes. With T- and B-enriched suspensions, virtually all T-lymphocytes were labelled with Po-anti-HTLA, whereas no B-cells were stained with this conjugate. The labelling was found to be irregularly distributed on the plasma membrane of T-cells. Direct identification with specific Po-anti-HTLA conjugate confirm the ultrastructural characteristics of thymus-dependant cells.This work was supported by I.N.S.E.R.M. grants No. 74-5-027-01 and A.T.P. No. 73-16.Acknowlegments. We are indebted toMartine Blanc who prepared the cell suspensions and toDanielle Germain who did the preparations for electron microscopic examination.     

The phylogenetic status of phyllomedusine frogs (hylidae) as evidenced from immunological studies of their serum albumins

Summary Based on immunological comparisons of the serum albumins of phyllomedusine frogs with both hyline and bufonid species, it is suggested that phyllomedusine frogs be erected to familial status within the superfamily Bufonoidea.This study was initiated in the Department of Biochemistry, University of California, Berkeley. Part of this work was supported by NSF grant No. DEB75-23543The author gratefully acknowledges the helpful advice and discussion ofA. C. Wilson. Thanks are also due toD. Wake, H. Cogger, W. Duellman andR. Heyer for generously supplying frog samples.     

Gilia in human fetal Schwann cells

Summary Cilia are present in Schwann cells during myelinogenesis which suggest that these cells could migrate by ciliary movement.Supported by U. S. PHS Grant No. 8-3360.Acknowledgment. I thank Drs.R. Allen, R. P. Bunge andR. A. Chambers for their advice and criticisms, and Mr.Alan Sandler for technical assistance.     

d-5-Chloro-2-(α-hydroxybenzyl)benzimidazole and 1-Alkyl-5-chloro-2-(α-hydroxybenzyl)benzimidazoles as inhibitors of poliovirus multiplication

Zusammenfassung Died-isomere Verbindung ist verantwortlich für die Poliovirus-hemmende Aktivität vondl-5-Chlor-2-(-oxy-benzyl)-benzimidazol.dl-1-Propyl-5-chlor-unddl-1-Butyl-5-chlor-Derivate sind ausserordentlich wirksam zur Verhinderung der Vermehrung der Typen 1, 2 und 3 des Poliovirus; andere 1-Alkyl-5-chlor-Derivate sind ebenfalls aktiv. Die 1-Alkyl-Grundverbindungen sind jedoch wirksamer als deren gleichartige 1-Alkyl-5-chlor-Derivate.

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The research is supported by the National Fund for Research into Poliomyelitis and other Crippling Diseases.     

Morphine suppression of ethanol withdrawal in mice

Summary The acute administration of morphine, alcohol or dopamine results in a pronounced suppression of the convulsions produced by alcohol in mice. The suppressive action of morphine on alcohol withdrawal in the mouse apparently is not a product of morphine intoxication, but rather to some other specific interaction between alcohol and morphine in the central nervous system. The conclusion suggest that dopamine may play a significant role as a modulator in convulsions produced during alcohol withdrawal.Dr.Kenneth Blum is Associate Professor in Pharmacology at The University of Texas Health Science Center at San Antonio and a Career Teacher in Drug Abuse and Alcoholism under a grant number 1-TO1-DA00290-01 from the National Institute on Drug Abuse.Acknowledgments. Our thanks are due toB. Wiggins, R. Marin andS. Elston for their excellent technical assistance. Research funded in part by Air Force Grant No. AFOSR-71-2075.     

Blood pyruvate in cats after hydrocortisone hemi-succinate

Zusammenfassung Hydrocortison - Na - hemi - Succinat (100 mg des Steroids) lebenden, 4 1/2 h fastenden Katzen injiziert, ergab sofortigen Anstieg der Pyruvat-Konzentrationen im Blut mit nachfolgendem Blutzuckeranstieg.Injektionen von Kontrollösungen ergaben keine Reaktion. Nach Steroidgaben erfolgte sowohl bei normalen wie adrenolektomierten Tieren ebenfalls Anstieg.

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I should like to thank Professors SirG. Pickering andI. E. Bush and Dr.R. V. Coxon for help and Mr.B. Abraham, MissS. Briers and Mr.W. Brown for technical assistance. Glaxo Laboratories Ltd. made a generous gift of the hydrocortisone-21-phosphate.     

Newton and the classical theory of probability

Summary Probabilistic ideas and methods from Newton's writings are discussed in § 1: Newton's ideas pertaining to the definition of probability, his probabilistic method in chronology, his probabilistic ideas and method in the theory of errors and his probabilistic reasonings on the system of the world. Newton's predecessors and his influence upon subsequent scholars are dealt with in §2: beginning with his predecessors the discussion continues with his contemporaries Arbuthnot and De Moiver, then Bentley. The section ends with Laplace, whose determinism is seen as a development of the Newtonian determinism.An addendum is devoted to Lambert's reasoning on randomness and to the influence of Darwin on statistics. A synopsis is attached at the end of the article.Abbreviations PT abridged Philosophical Transactions of the Royal Society 1665–1800 abridged. London, 1809 - Todhunter I. Todhunter, History of the mathematical theory of probability, Cambridge, 1865 To the memory of my mother, Sophia Sheynin (1900–1970)     

The effect of the ergoline derivative VUFB-6683 on the adenohypophysial prolactin concentration in rats

Zusammenfassung Mit Hilfe vond-6-Methyl-8-ergolin-I-ylacetamid-Tartarat, VUFB-6683 wurde bei säugenden Ratten das Gewicht und der Prolaktinspiegel der Adenohypophyse herabgesetzt und die Laktation gehemmt.

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The authors are indebted to Dr.I. J. Skála, Dr.J. Hondlík, Mrs.V. Maitová and Mrs.J. Emanuelová for technical assistance; and to Dr.I. Mikulá for his aid in designing the study.