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.     

A new one-step synthesis of hexahydrocannabinoid analogs

Summary A one-step synthesis of hexahydrocannabinoid analogs (HHC) is described making use of the condensation of phenolic ketones and aldehydes with citronellal in the presence of pyridine.Grateful thanks are accorded to Drs L. Chopard and S. Selvavinayakam for spectral measurements and Dr I. Fleming for useful discussion.R. Mechoulam and Y. Gaoni, Recent advances in the chemistry of Hashish, in: Progress in the Chemistry of Organic natural products, vol. 25, p. 175. Ed. L. Zechmeister. Springer Verlag, Wien 1967; R. Mechoulam, Marijuana Chemistry and Pharmacology, metabolism and clinical effects. Academic Press, New York 1973; R. Mechoulam, N. K. McCallum and S. Burstein, Chem. Rev.76, 75 (1976).     

Insulin stimulation of glucose and amino acid transport in mouse fibroblasts with elevated membrane microviscosity

Summary Basal and insulin-stimulated transport of 2-deoxy glucose and of -aminoisobutyric acid in mouse 3T3 fibroblasts were modulated by increasing the lipid microviscosity of the cell plasma membrane. The kinetics indicate that the insulin effect is induced either by recruitment of new transport carriers or by reduction of the translocation activation energy.This investigation was supported by grant No.5-R01-CA-27471-02, awarded by the National Cancer Institute, Department of Health, Education and Welfare.     

Blocking by picrotoxin of nigra-evoked inhibition of neurons of ventromedial nucleus of the thalamus

Summary The transmitter substance released by nigro-thalamic fibres is proposed to be -aminobutyric acid, since picrotoxin blocked nigra-evoked monosynaptic inhibition of thalamic neurons.Supported by grants Nos 212009 and 311410 from Ministry of Education of Japan.The authors wish to thank Dr Marjorie Anderson, University of Washington, Seattle, for improving the English.     

Comparative study, in the Allium test, of the cytotoxicity of tubulosine and of 6 synthetized pseudo-tubulosines]

Comparing cytotoxicity of tubulosine and of six newly synthesized pseudo-tubulosines in the Allium test, we have characterized all the current features of protein inhibition. Nevertheless cytotoxicity of the six pseudotubulosines is much weaker. Furthermore, "floating poles anaphasis", a disturbance characteristic of the action of tubulosine, has been found with a lesser intensity with the other compounds.     

The effects of physostigmine on the oxygen uptake in rat brain tissue

Summary Physostigmine in a dose of 0.1 mg/kg i.v. expressly stimulated the oxygen uptake in the rat cerebral cortex. This effect was blocked by propranolol and seems be mediated by catecholamines. Since atropine also antagonized the stimulant effect of physostigmine, it appears that the action of physostigmine is primarily cholinergic and that the adrenergic effect is a secondary phenomenon. The higher dose of physostigmine (0.4 mg/kg i.v.) caused a depression of rat brain oxygen uptake.This work was supported by a grant from Serbian Republic Scientific Fund (ZMNU SR Srbija), Belgrade (Yugoslavia).The authors wish to acknowledge the skilful technical assistance of Lj. Krsti.     

(−)-Maalian-5-ol,a new enantiomeric sesquiterpenoid from the liverwortPlagiochila ovalifolia

Summary A new enantiomeric sesquiterpene alcohol named (–)-maalian-5-ol was isolated from the liverwort, and the structure and absolute configuration was determined to be the stereostructureI by chemical and spectral evidence.The authors express their gratitude to Dr H. Inoue, National Science Museum, for identification of the liverwort, and Prof. T. Tokoroyama, Osaka City University, for sending of the data of (–)--maaliene and (+)-selina-5,11-diene. Thanks are also due to the Ministry of Education for financial support of this work.     

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.     

Lysergic acid diethylamide affects blood flow to specific areas of the conscious rat brain

Zusammenfassung Die i.v. Verabreichung von LSD an Ratten steigert den Blutkreislauf im Hirnstamm sowie im frontalen und parietalen Cortex selektiv. Es wurden durch 6-Nor-LSD, 2-Methyl-LSD und ^{8, 9}-LSD weder wahrnehmbare Verhaltensänderungen noch Änderungen des regionalen Blutkreislaufs verursacht.