Effect of AD6 (8-monochloro-3-beta-diethylamino-ethyl-4-methyl-7-ethoxycarbonylmethoxy coumarin) on cyclic nucleotide phosphodiesterases in human platelets

Summary The effect of AD6 (8-monochloro-3-beta-diethylamino-ethyl-4-methyl-7-ethoxycarbonylmethoxy coumarin), an inhibitor of platelet aggregation, on cyclic nucleotide metabolism was investigated. AD6 inhibited selectively human platelet cyclic GMP phosphodiesterase, which was separated from cyclic AMP phosphodiesterase by DEAE-cellulose chromatography. Addition of AD6 to washed platelets increased cyclic GMP levels significantly in two minutes. These results could be useful in elucidating the action of AD6 on intact platelets.     

7-Chloro-3-(4-methyl-1-piperazinyl)-4H-1,2,4-benzothiadiazine-1,1-dioxide a new antihypertensive agent

Summary 7-Chloro-3-(4-methyl-1-piperazinyl)-4H-1,2,4-benzothiadiazine-1,1-dioxide (DU-717) is a new compound having sustained antihypertensive activity in a similar manner to that of hydrochlorothiazide. However, this compound shows neither diuretic nor hyperglycemic effect, being different from those of hydrochlorothiazide or diazoxide.     

Structure-activity relationship of various acyl derivatives of 6-methyl-8β-aminomethyl-10α-ergoline (dihydrolysergamine)

Riassunto Alcuni acil derivati dell'ergoline hanno dimostrato notevoli proprietà ossitociche, adrenolitiche ed anti-5-idrossitriptaminiche, (anti-5-HT). In particolare l'acetil e l'isobutirril diidrolisergamina possiedono una azione ossitocica altrettanto potente e più elettiva dell'ergometrina, della quale sono anche meno tossiche.     

Isolation and some properties of the heparin-neutralizing factor (PF4) released from human blood platelets

Zusammenfassung Der in Form eines hochmolekularen Komplexes von den Plättchen freigesetzte, heparinneutralisierende Faktor (PF 4) konnte reversibel in ein Träger-Material und ein aktives Protein (Molekulargewicht ca. 30000) aufgespalten werden.

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This work was supported by the Schweizerischer Nationalfonds zur Förderung der wissenschaftlichen Forschung.     

Effect of sodium butyrate in combination with prostaglandin E1 and inhibitors of cyclic nucleotide phosphodiesterase on human amelanotic melanoma cells in culture

Summary Sodium butyrate and cyclic AMP-stimulating agents (prostaglandin E₁, papaverine, theophylline, and RO20-1724) caused reductions in the cell number (primarily due to reduction in cell division) when added individually to human melanoma cells in culture. However, the combination of sodium butyrate with one of the cyclic AMP-stimulating agents produced a marked reduction in cell number (primarily due to cell death).Supported in part by BRSG grant RR-05357 awarded by Biomedical Research Support Grant Program, Division of Research Resources, National Institutes of Health. We thank Marianne Gaschler for her technical help.     

Effect of sodium butyrate in combination with prostaglandin E1 and inhibitors of cyclic nucleotide phosphodiesterase on human amelanotic melanoma cells in culture.

Sodium butyrate and cyclic AMP-stimulating agents (prostaglandin E1, papaverine, theophylline, and RO20-1724) caused reductions in the cell number (primarily due to reduction in cell division) when added individually to human melanoma cells in culture. However, the combination of sodium butyrate with one of the cyclic AMP-stimulating agents produced a marked reduction in cell number (primarily due to cell death).     

Effect of N-6 2'-O-dibutyryl adenosine 3'-5'monophosphate (dibutyryl cyclic AMP) on the condenstion of the X chromosome into the form of a Barr body]

Addition of exogen DB-c AMP in medium of human fibroblasts culture, with 46 XX karyotypes, enables us to observe a high frequency of Barr bodies, about 80 or 85%. This observation suggests that the condensation of the X chromosome in the form of Barr bodies depends on the level of endogen cyclic AMP.     

Effect of N6O2-dibutyryl cyclic 3′,5′-adenosine monophosphate on the pinocytosis of brain capillaries of mice

Zusammenfassung Die Anzahl der pinocytotischen und stachligen Vesicula wurde unter normalen Bedingungen mit Bezug auf einheitliche Gebiete der pinocytotischen Aktivität der Kapillaren von Mäusegehirnen quantitativ charakterisiert. Die Pinocytose der Gehirnkapillaren war durch das substitutielle cyclische N⁶O²-Dibutyrylderivat des 3,5-Adenosinmonophosphats signifikant gesteigert.     

The absence of an inhibitory effect of metyrapone (2-methyl-1,2-di (3-pyridyl) propan-1-one) on hepatic microsomal hydroxylation in scurvy

Summary Microsomes from livers of scorbutic guineapigs showed a reduced rate of acetanilide hydroxylation. The response of scorbutic liver microsomes to the inhibitor Metyrapone (2-methyl-1,2 di (3-pyridyl)propan-1-one) was different from that of liver microsomes from non-scorbutic guinea-pigs.