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.     

Modulation of an ‘equilibrium enzyme’: Ecological evidence

Summary The activity of D-lactate dehydrogenase in the foot of the snail,Helix pomatia, is closely correlated with time of year and mean daily temperature, and increases strikingly after the animals have been exposed to a nitrogen atmosphere for 24 h.I thank U. Platzer for technical assistance and D. Frank for help with the statistics. The investigation was supported by the Fonds zur Förderung der wissenschaftlichen Forschung in Österreich, project No. 1257 and 2919.     

Chemotherapeutic effects of 4-isothiocyanato-4′-nitrodiphenylamine (C9333-Go/CGP 4540) on infections withNematospiroides dubius,Hymenolepis diminuta,Hymenolepis nana andSpirometra mansonoides

Summary 4-Isothiocyanato-4-nitrodiphenylamine possessed anthelmintic activity againstNippostrongylus dubius andHymenolepis nana in mice andH. diminuta in rats as determined by both egg counts and recovery of parasites at autopsy. No activity was detected against the cestode,Spirometra mansonoides, in cats.This investigation was supported in part by grants AI-10512 and AI-09483 from the National Institutes of Health. The authors are indebted to Dr P.P. Weinstein for providing animals infected withSpirometra mansonoides.     

The detection of superoxide anion from the reaction of oxyhemoglobin and phenylhydrazine using EPR spectroscopy

Summary The low temperature EPR spectrum of a quickly reacted mixture of oxyhemoglobin and phenylhydrazine was studied. With the use of a computer, the spectral contribution of methemoglobin in the region of g=2 was subtracted. The remaining spectrum was that of an axial free radical (g=2.00, g=2.06) having the magnetic parameters of superoxide anion. In the presence of superoxide dismutase, this axial radical was not seen, confirming that superoxide anion is indeed generated by the reaction.The portion of this investigation carried out at the Albert Einstein College of Medicine was supported in part by US Public Health Service Research Grant HL-93399 from the Heart and Lung Institute and by National Institute Contract Nol-CP-55606 to J.P. This is communication No. 378 from the Joan and Lester Avnet Institute of Molecular Biology.Predoctoral fellow in the Medical Scientist Training Program (United States Public Health Service Grant 5-TO-5-GM 01669-12) at the New York University School of Medicine.Recipient of a grant-in-aid from the New York Heart Association.     

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.     

Struktur-Wirkungsbeziehungen beim menschlichen Calcitonin. III. Die biologische Aktivität verkürzter oder an den Kettenenden modifizierter,synthetischer analoger

Summary Assays of 8 synthetic analogues of human calcitonin in rats showed that their hypocalcaemic activity was drastically reduced by deletion of the C-terminal amide group, chain-shortening or opening of the disulphide ring, but unaffected or enhanced by modification of the N-terminal amino group.

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II. vgl.R. Maier, B. Kamber, B. Riniker andW. Rittel, Hormon. Metab. Res.7, 511 (1975).

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Die hier verwendete, abgekürzte Schreibweise für Peptide folgt den Empfehlungen der IUPAC-IUB Kommission für Biochemische Nomenklatur, J.B.C.247, 977 (1972). Weitere Abkürzungen: HCT, Human-Calcitonin; PCT, Schweinecalcitonin; Bmp, -Mercaptopropionsäure (Desaminocystein); NMet, Normethionin (S-Methylcystein); -OMe, Methylester.     

Ecdysone 20-hydroxylase from the midgut of the tobacco hornworm (Manduca sexta L.)

Summary An ecdysone 20-hydroxylase enzyme system that converts -ecdysone to 20-hydroxyecdysone was prepared from the midgut of the tobacco hornworm prepupa. This partially purified enzyme is NADPH dependent and is localized in the mitochondrial fraction of the midgut tissue.