A cannabinoid with cardiovascular activity but no overt behavioral effects

Summary Abnormal-⁸-tetrahydrocannabidiol (ABN-⁸-THC) failed to elicit central nervous system and cardiovascular effects in laboratory animals. Abnormal-cannabidiol (ABN-CBD) was also devoid of overt behavioral effects but produced marked hypotension with only slight bradycardia in anesthesized dogs.Acknowledgment. This work was supported by NIDA (grant No. DA-00574-01 and DA-00490) and Virginia Heart Society (grant No. RR-05697)     

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).     

Antioxidant effects on prostaglandin synthesis in rabbit kidney medulla slices

Summary Sodium diethyldithiocarbamate, 2,6-di-tert-butylphenol and N,N-diphenyl-p-phenylenediamine inhibited the generation of medullary prostaglandin E, but 1,2-dimethoxyethane (OH scavenger) and 2,5-dimethylfuran (¹O₂ scavenger) stimulated basal prostaglandin E production 1.2–1.3-fold. These results suggest that the balance between formation and removal of cellular lipid peroxides sets a peroxide level that can regulate the rate of prostaglandin formation in cells.     

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.     

Occurrence of Hyp3-bradykinin in methanol extracts of the skin of the South African leptodactylid frogHeleophryne purcelli

Summary Methanol extracts of the skin of the South African amphibians belonging to the genusHeleophryne (H. purcelli purcelli, H. purcelli depressa, H. purcelli orientalis, H. natalensis) contain large amounts (20–500 g/g fresh tissue) of Hyp³-bradykinin.Supported by grants from the Consiglio Nazionale delle Ricerche, Italy, and from the Ministry of Education, Japan.     

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.     

Leydig cell function in streptozotocin-induced diabetic rats.

Streptozotocin diabetic rats were infertile as a result of decreased Leydig cell function of the testes. The major changes found were: decreased number of Leydig cells and their spontaneous secretion of testosterone. No change in the receptors to LH on the Leydig cells was observed. LH was found to be obligatory for the regulation of Leydig cell function and fertility.     

Alkaline phosphatase in human lymphocyte subpopulations.

The levels of membrane alkaline phosphatase have been measured on different lymphocyte fractions from human peripheral blood separated on bovine serum albumin discontinuous gradients. The peak in enzyme activity was observed in a non-T-, non-B-cell fraction, rich in "null" lymphocytes; the lowest values were found in the fraction with the highest proportion of T-cells.