H. J. Bein

Bio: H. J. Bein is an academic researcher from Ciba Specialty Chemicals. The author has contributed to research in topics: Hexamethonium & Efferent. The author has an hindex of 7, co-authored 10 publications receiving 419 citations.

Reserpin, der sedative Wirkstoff ausRauwolfia serpentina Benth

Abstract: The sedative principle ofRauwolfia serpentina Benth. has been isolated in pure crystalline form and its chemistry and pharmacology has been studied.

Zur Pharmakologie des Reserpin, eines neuen Alkaloids ausRauwolfia Serpentina Benth

Abstract: Reserpin, a new, highly active alcaloid fromRauwolfia serpentina benth., shows a very marked hypnotic effect and lowers the blood pressure.

The antitoxic effect of aldosterone

Abstract: Aldosteron schutzt bei verschiedenen Tierarten — als wirksamstes aller untersuchten Corticosteroide — gegenuber verschiedenartig ausgelosten «Schockzustanden». Bei der Katze normalisiert es die durch Endotoxine veranderte vaskulare Reaktivitat gegenuber Adrenalin und Nor-Adrenalin. Es ist moglich, dass im Endotoxin-Schock die Konzentration von Nor-Adrenalin unterschwellig wird, und dass seine Wirkung, eventl. auch Freisetzung, von Aldosteron abhangt.

Zur Pharmakologie des N,N,N′,N′-3-Pentamethyl-N,N′-diäthyl-3-aza-pentan-1,5-diammonium-dibromid (Ciba 9295), einer ganglionär hemmenden Substanz

Abstract: N,N,N′,N′-3-pentamethyl-N,N′-diethyl-3-aza-pentane-1,5-diammonium-dibromide, CIBA 9295, is a potent and specific ganglionic blocking agent in a concentration of less than a 1/1000 of the acute toxic dosage. A comparison with the well known ganglionic blocker, tetra-ethylammonium bromide, shows 9295 to be less toxic, more effective and possessing a more prolonged duration of action.

Mechanism of action of glucocorticoids.

Abstract: The mechanism of action of glucocorticoids is reviewed from the standpoint of seeing how far current concepts of the molecular action of steroids go towards explaining the varied physiologic and metabolic effects induced. The role of plasma binding to transport proteins in modifying steroid action is considered. The interactions between glucocorticoids and other hormones, particularly those mediated by cAMP are considered along with a discussion of the mechanism of “permissive” effects. Various proposals concerning the way in which glucocorticoids induce their effects including direct interactions with enzymes, nucleic acids, lysosomes, and receptor proteins are considered in detail, and an attempt is made to consider how far each of these mechanisms can go in explaining steroid action. Those biologic effects that cannot be accounted for by currently available mechansims are mentioned. Effects of glucocorticoids on growth, differentiation, and the inflammatory response are discussed from a mechanistic point of view. Catabolic or inhibitory effects of glucocorticoids as well as enzyme induction are examined using several exemplary systems. Finally an attempt is made to summarize the current state of knowledge concerning glucocorticoid and genome interaction.

Small molecule natural products in the discovery of therapeutic agents: the synthesis connection.

Abstract: Natural products have been a rich source of agents of value in medicine. They have also inspired, at various levels, the fashioning of nonnatural agents of pharmaceutical import. Hitherto, these nonnatural derivatives have been primarily synthesized by manipulating the natural product. As a consequence of major innovations in the subscience of synthetic methodology, the capacity of synthesis to deal with molecules of considerable complexity has increased dramatically. In this paper, we show by example some total syntheses which draw from strategy-enabling advances in methodology. Moreover, we show how these capabilities can be used to discover and develop new agents of potential pharmaceutical value without recourse to the natural product itself.

Drugs which block the storage of 5-hydroxytryptamine and related amines

Abstract: In 1955 Shore, Brodie and coworkers (Shore, Silver and Brodie 1955, Pletscher, Shore and Brodie 1955) discovered that reserpine caused a marked decrease in the concentration of 5-hydroxytryptamine (5-HT) in tissues and a concomitant rise in the urinary excretion of the 5-HT metabolite 5-hydroxyindoleacetic acid. The deep physiological significance of this discovery became even more evident when reserpine soon afterwards was found to affect tissue catecholamines in a similar manner, an effect leading to block of adrenergic transmission mechanisms (Carlsson and Hillarp 1956a, Bertler, Carlsson and Rosengren 1956). Since then numerous papers have appeared, in which the effects of Rauwolfia alkaloids and a group of similarly acting benzoquinolizines (Pletscher, Besendorf and Bachtold 1958) have been further analyzed. Particular interest has been focussed on the mechanism of action on the abovementioned amines and on the relationship between this action and the various pharmacological effects of Rauwolfia alkaloids and benzoquinolizines. It is the aim of the present Chapter to review and discuss the pertinent literature dealing with these fundamental problems rather than to review in detail the enormous literature on the pharmacology of these agents.

History of the discovery and clinical introduction of chlorpromazine

Abstract: Background. The historical process of discovery and clinical introduction of chlorpromazine, one of the greatest advances of 20th century medicine and history of psychiatry, is analyzed.Methods. In this review, we have studied the original works of pioneers in the discovery and clinical use of chlorpromazine, as well as the contributions of prestigious researchers (historians, pharmacologists, psychiatrists, etc.) about this topic.Results. The discovery of phenothiazines, the first family of antipsychotic agents has its origin in the development of German dye industry, at the end of the 19th century (Graebe, Liebermann, Bernthsen). Up to 1940 they were employed as antiseptics, antihelminthics and antimalarials (Ehrlich, Schulemann, Gilman). Finally, in the context of research on antihistaminic substances in France after World War II (Bovet, Halpern, Ducrot) the chlorpromazine was synthesized at Rhone-Poulenc Laboratories (Charpentier, Courvoisier, Koetschet) in December 1950. Its introduction in anaesthes...