New dopamine receptor stimulant drug

Zusammenfassung Es wird der Nachweis erbracht, dass2(p-nitrobenzylthio)-Imidazolin (3H) · HCl (NBTI) Dopamin-Rezeptoren von Mäusen, Ratten und Affen direkt zu stimulieren vermag.

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The authors wish to thank Dr.G. Ullyot, SKF Laboratories, for gifts of NBTI and chlorpromazine; Dr.H. Corrodi, AB Hässle, Göteborg, Sweden, for the methyl ester hydrochlorides ofl-Dopa,-methyl-p-tyrosine andp-chlorophenylalanine; McNeil Laboratories, Inc., Fort Washington, Pennsylvania, for the haloperidol; and Schering Corporation, Bloomfield New Jersey, for perphenazine. Thanks are also due toA. Schindler for his skillful technical assistance.

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Final paper in press, Eur. J. Pharmac. (1972).     

Glucocorticoids suppress cystathionine gamma-lyase expression and H2S production in lipopolysaccharide-treated macrophages

Hydrogen sulfide (H₂S) plays an important role in inflammation. We showed that macrophages expressed the H₂S-forming enzyme cystathionine gamma-lyase (CSE) and produced H₂S. Lipopolysaccharide (LPS) stimulated the CSE expression and H₂S production rate. l-cysteine reduced LPS-induced nitric oxide (NO) production. CSE inhibitor blocked the inhibitory effect of l-cysteine. CSE knockdown increased, whereas CSE overexpression decreased LPS-induced NO production. Dexamethasone suppressed LPS-induced CSE expression and the H₂S production rate as well as NO production. l-arginine increased, whereas N^G-nitro-l-arginine methyl ester (l-NAME) decreased LPS-induced CSE expression and H₂S production. Dexamethasone plus l-NAME significantly decreased LPS-induced CSE expression and H₂S production compared to l-NAME. Our results suggest that macrophages are one of the H₂S producing sources. H₂S might exert anti-inflammatory effects by inhibiting NO production. Dexamethasone may directly inhibit CSE expression and H₂S production, besides the NO-dependent way. Inhibition of H₂S and NO production may be a mechanism by which glucocorticoids coordinate the balance between pro- and anti-inflammatory mediators during inflammation.     

Catalytic properties of synthetic pentapeptides

Zusammenfassung Es wurde das Pentapeptidl-Thr-l-Ala-l-Abu-l-His-l-Asp synthetisiert, seine katalytische-hydrolytische Wirkung auf Essigsäure-p-nitrophenylester geprÜft und die katalytische Aktivität ca. 1/3 derjenigen seines isosterenl-Thr-l-Ala-l-Cys-l-His-l-Asp festgestellt.

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Work done on a leave of absence from the Research Council of Alberta, Canada.     

The isolation and amino acid sequences of new pyroglutamylpeptides from snake venoms

Zusammenfassung Die Strukturaufklärung von zwei neuen tryptophanhaltigen Peptiden im Schlangengift vonAgkistrodon halys blomhoffii ergeben:l-Pyroglutamyl-l-Glutaminyl-l-Tryptophan undl-Pyroglutamyl-l-Asparaginyl-l-Tryptophan. Diese Peptide sind in Schlangengiften der Viperidae- und Crotalidae-Arten verbreitet.

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Supported in part by a grant from the Ministry of Education (Japan).     

Diketopiperazines containing L-proline from Streptomyces lavendulae and their stereochemistry in solution

Summary l-Valyl-l-proline (I),l-leucyl-l-proline (II),l-phenylalanyl-l-proline (III) andl-isoleucyl-l-proline (IV) anhydrides were isolated from the cultures ofStreptomyces lavendulae No. 314 and, on the basis of¹³C-NMR and CD spectra, their stereochemistry in solution is described.Acknowledgments. The authors would like to express their sincere thanks to Prof. H. Ogura, Kitasato University, for kind supply of the authenticl-valyl-l-proline anhydride and to Mr. A. Takakuwa, JASCO, for measuring the CD curves with J-40 automatic recording spectropolarimeter.     

Über den Einbau von Dipeptiden in Ergotoxin-Alkaloide

Summary l-Valyl-l-leucine-U-¹⁴C,l-valyl-l-proline-U-¹⁴C-lactam andl-leucyl-l-proline-U-¹⁴C-lactam were administered to submerged cultures of an ergotoxine-mixture-producing strain ofClaviceps purpurea. The added dipeptides were split by the fungus into the corresponding amino acids prior to incorporation. Apparently dipeptides are no immediate precursors for the peptide side-chain of ergotoxinealkaloids.     

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.     

β-Pyrrolo-L-alanine,a new antimetabolite of phenylalanine and tyrosine inEscherichia coli

Zusammenfassung -Pyrrolo-l-alanin, dessen Synthese beschrieben ist, hemmt das Wachstum vonE. coli B auf synthetischen Nährböden. Die Hemmung wird vonl-Phenylalanin undl-Tyrosin vollständig, vonl-Tryptophan teilweise, nicht aber von Histidin aufgehoben. Stämme vonE. coli, die gegen-Pyrrolo-l-alanin bzw.p-Fluorophenyl-dl-alanin resistent sind, zeigen gekreuzte Resistenz.     

Synthesis and structure of Fungisporin

Zusammenfassung Die Struktur von Fungisporin, eines Zyklopeptides aus Sporen verschiedener Spezies vonPenicillium undAspergillus-Arten, wird durch Synthese und Vergleich mit dem Naturprodukt als die eines Zyklotetrapeptides, cyclo-(l-Phe-d-Val-l-Val-d-Phe-), bewiesen.     

Zur leukotaktischen Wirkung von Aminosäuren in Liquor cerebrospinalis

Summary Intercisternal injections of-aminobutyric acid,l-asparagin,l-glutamine,l-leucine andl-norleucine exert a strong leukotactic action and in dogs result after a short time in a maximum cell increase of 76,000/3 cells.     

A comparison ofl-asparaginase fromErwinia aroideae and fromEscherichia coli: Biochemical and biological properties

Zusammenfassung l-Asparaginase wurde ausErwinia aroideae gewonnen und durch Fraktionierung wie Fällungsschritte und Chromatographie um das 500fache angereichert. Das Enzym zeigt keine immunologische Kreuzreaktion mitl-Asparaginase ausEscherichia coli. Durch Acylierung lässt sich das basische Proteinl-Asparaginase ausE. aroideae in ein saures Protein unter weitgehendem Erhalt der Enzymaktivität überführen.     

A modified dipeptide from the algaCystoseira corniculata hauck

Summary A modifiedl-Phe-l-Phe dipeptide has been isolated from the algaCystoseira corniculata.We thank ProfessorK. C. Güven, Botanical Institute, University of Istanbul, for collecting the alga.     

Ein neues Alkaloid aus dem Mycel einesClaviceps purpurea-Stammes. Zur Biogenese von Ergocristin

Summary A new alkaloid from the lyophilized mycelia of aClaviceps purpurea strain, N-[N-(d-Lysergyl)-l-valyl]-l-phenylalanyl-d-prolin-lactam, has been isolated and characterized. From its fast methanolysis it is deduced that the previously reported N-(d-Lysergyl)-l-valinmethylester is actually an artefact. The biogenetic significance and its possible role in biogenesis of Ergocristine is discussed.     

Über das Verhalten der optischen Isomeren von Adrenalin im Blut

Summary Demethylation ofl- andd-adrenaline was studied on narcotized catsin vivo.In metabolism of infusedl-adrenaline, formation of noradrenaline represents one first step.On the other hand, metabolism ofd-adrenaline does not show any intermediate formation of noradrenaline.     

Inhibition of L-Alanine-induced germination ofBacillus cereus spores by theophylline

Riassunto In spore diBacillus cereus, la teofillina inibisce reversibilmente la germinazione dal-alanina ma non l'attivazione che lal-alanina esercita sulla germinazione da inosina. Il possibile significato di questi dati è discusso.     

On the structure of the natural dipeptide N-acetyl-aspartyl-glutamic acid (NAAGA)

Riassunto Si descrive la sintesi dei due dipeptidi isomeri acido N-acetil--l-aspartil-l-glutammico (I) e acido N-acetil--l-aspartil-l-glutammico (II). Il loro confronto con il NAAGA, dipeptide precedentemente isolato dal tessuto nervoso di alcuni mammiferi, ha dimostrato l'identità del nuovo metabolita con il-dipeptide (II).     

Zur Pharmakologie von Convallatoxol,zugleich ein Beitrag zur pharmakologischen Strukturanalyse von g-Strophanthin

Summary A report is given of the positive inotrope effects of genins and glycosides with one methyl or aldehyde or carbinol group in the C₁₀ atom of the steroid stage, and of the influence of thel-rhamnose compared withd-digitoxose andd-cymarose. A structure analysis of the ouabain and convallatoxol is derived from the differences in the degree of abolition of the acute cardiac damage in the experiments.     

Female sex pheromone of the longhorn beetleMigdolus fryanus Westwood: N-(2′S)-methylbutanoyl 2-methylbutylamine

The first known long-range female-released sex pheromone for the family Cerambycidae is reported fromMigdolus fryanus, a sugarcane pest in South America. Although two female-specific compounds, namely, N-(2S)-methylbutanoyl 2-methylbutylamine and N-formyll-isoleucine methyl esters were identified, field tests with synthetic chemicals revealed that only the amide was active and that the amino acid derivative neither increased or decreased trap catches by the amide. This is the first identification of amide as a sex pheromone.