In vivo effects of Escherichia coli endotoxin on sulfobromophthalein clearance in the guinea-pig.

In vivo studies indicated that the primary effects of E. coli endotoxin on hepatic clearance of sulfobromophthalein were at the excretory level. Newborns were more sensitive to the LPS than older animals.     

A facile one-step synthesis of cysteinyldopas using mushroom tyrosinase

Summary A convenient one-step procedure, based upon the tyrosinase co-oxidation of dopa and cysteine, is reported for the synthesis of 5-S-cysteinyldopa (I) in 74% yield. Secondary products of the reaction turned out to be 2-S-cysteinyldopa (II, 14%), 2,5-S, S-dicysteinyldopa (IV, 5%), and the hitherto unknown 6-S-cysteinyldopa (III, 1%).The generic term cysteinyldopa is proposed to designate the various cotechol amino-acids arising from addition of cysteine to dopaquinone.This work was supported in part by a grant from Consiglio Nazionale delle Ricerche, Roma.     

Some properties of the goat placental lactogen

Summary Goat placental lactogen was partially purified from a medium collected after placental tissue incubation. The data obtained by disc electrophoresis and isoelectric focusing experiments, as well as by means of radioreceptor assay methods, provide evidence of the similarity between the goat and ovine placental lactogen.The careful technical assistance of L. Tichovská is gratefuly acknowledged.     

An electrophoretic investigation of the binding of 3-14C coumarin to rat serum proteins

Summary The binding of coumarin to serum proteins of the rat has been demonstrated. Of the total bound coumarin (37% of injected dose), 36% was bound to the slow and fast ₁ globulins, 11% to the post albumins, 10% to globulin and 9% to albumin.     

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.     

Influence of PGA1 on cartilage growth

Summary Using the Fell technique of organ culture of cartilage in a chemically defined medium, it has been shown that prostaglandin A₁ at a concentration of 25 g/ml caused chondrocyte death in chick embryonic limb rudiments. An equimolar concentration of PGE₂ was not toxic to the cells.Acknowledgments. We are grateful for the support of C. J. K. by the Medical Research Council and of D. L. G. by the Arthritis and Rheumatism Council for Research. Our thanks are due to Dame Honor Fell, F. R. S. for invaluable advice and guidance, to Dr J. Pike (Upjohn Co.) for supplies of prostaglandin A₁, and to Dr Sylvia Fitton-Jackson for the gift of culture medium.     

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).     

Starfish saponins. Part 101. Further 24-O-glycosidated steroids from the starfishHacelia attenuata

Summary On the basis of comparative spectral data, the structures of 3 novel steroidal glycosides from the Mediterranean starfishHacelia attenuata have been elucidated as3, 4 and5. These are further examples of a novel group of 24-O-glycosidated steroids recently encountered in the same species and in the Pacific speciesProtoreaster nodosus.Part 9. L. Minale, C. Pizza, R. Riccio and F. Zollo, Experientia39 (1983) 567. This contribution is part of the Progetto Finalizzato Chimica fine e secondaria del C.N.R., Roma.Acknowledgments. We thank Prof. K. Nakanishi, Columbia University, New York, for FD-mass spectral analyses, the Centro Interfacoltà di Metodologie Chimico-Fisiche for 270 MHz NMR facilities, and Miss R. Aquino for part of the experimental work.