Model of the effect of 4-aminopyridine at the level of potassium channels of the giant axon of the squid, Logigo forbesi L.]

Most of the effects of 4-aminopyridine on the potassium conductance of the giant axon of the Squid can be explained in terms of a simple model based on the physicochemical properties of the molecule and what is known about the structure of the potassium "channels".     

X-ray analysis of Co-C bond cleavage in the crystalline state

During serial structure analysis of cobaloxime derivatives, aimed at interpreting the catalytic capability of the asymmetric hydrogenation, we have found that the crystal of R-alpha-cyanoethyl (S-alpha-methylbenzylamine)-cobaloxime changes its unit cell dimensions by X-ray exposure without degradation of a single crystal form. The rate of the change was so slow that it was possible to collect the intensity data for several intermediate stages. We have proved, by calculating electron density in each stage, that the change reflects the racemisation of the cyanoethyl group.     

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).     

Proteolytic activity on endogeneous substrates in cell-free extracts ofTrypanosoma cruzi

Summary Cell-free extracts ofTrypanosoma cruzi contain proteolytic activity able to degrade endogenous substrates. The activity was maximal at pH 3 to 4, had an optimal temperature of 65°C, and was strongly inhibited by N--p-tosyl-L-lysine chloromethyl ketone.This investigation received financial support from the UNDP/World Bank/WHO Special Programme for Research and Training in Tropical Diseases, the Fundación Julio Cherny, and the Ministerio de Salud Pública y Medio Ambiente de la República Argentina. The authors gratefully acknowledge the technical assistance of Mr Esteban Bontempi.     

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.     

Effects of several preoperative medications on fat cell lipolysis, and activity of adipose tissue cyclic AMP phosphodiesterase.

Effects were examined of atropine, diazepam, pethidene, promethazine, scopolamine, omnopon and papaverine on basal and noradrenaline-stimulated lipolysis in rat isolated fat cells and on rat adipose tissue cyclic AMP phosphodiesterase activity. Papaverine at high concentration (1 mM) inhibited both basal and hormone-stimulated lipolysis, whereas diazepam enhanced basal lipolysis. At a 'clinical dose', omnopon increased both basal and noradrenaline-stimulated lipolysis. Adipose tissue cAMP phosphodiesterase activity was strongly inhibited by 1 mM diazepam, papaverine, promethazine and omnopon (280 microgram ml-1). Lack of enhancement of lipolysis by the established cAMP phosphodiesterase antagonist papaverine, is compatible with simultaneous inhibition also of adipose adenyl cyclase. Diazepam-stimulated lipolysis is compatible with its phosphodiesterase inhibitory activity. It is proposed that papaverine-containing omnopon may offer some survival advantages during surgical stress by facilitating a caloric supply.     

Multiplicity of monoamine oxidase in chick brain

Summary The substrate- and inhibitor-related characteristics of monoamine oxidase (MAO) were studied on chick brain mitochondria. It was found that neither 5-hydroxytryptamine nor -phenylethylamine is the specific substrate for type A and type B MAO in chick brain.