A method for the fluorimetric determination of 4-(2-Hydroxy-3-isopropylaminopropoxy)-indole (LB 46), aβ-blocking agent,in plasma and urine

Zusammenfassung Eine empfindliche fluorimetrische Methode zur Bestimmung von 4-(2-Hydroxy-3-isopropylaminopropoxy)-indol, dem-Blocker LB 46, in Plasma (Erfassungsgrenze 0,02 g) und in Urin (Erfassungsgrenze 0,05 g) wird beschrieben. Die mit dieser Methode gemessene biologische Halbwertszeit im Plasma beträgt nach peroraler Verabreichung beim Menschen 3 h und bei der Ratte etwa 30 min.     

Beta-adrenergic blocking effect of dichloroisoprenaline (DCI), (H 56/28, I.C.I. 50172, LB 46), methoxamine (MJ 1999) and propranolol on the sinus node activity of the dog heart

Zusammenfassung Der Hemmungseffekt sieben-adrenergischer Blockierungsmittel auf positive chronotrope Wirkung bei zunehmender Dosierung von Isoprenalin wurde durch Verabreichung in die Sinusknotenarterie vergleichend untersucht. Reihenfolge der Wirksamkeit: LB 46, H 56/28, Propranolol>I.C.I. 50172, DCI>MJ 1999>Methoxamin.     

Synthesis of the anomeric 9-(2-deoxy-1-D-glucosyl)-adenines and their anhydro derivatives

Zusammenfassung Synthesen von 9-(2-Deoxy-1-D-glukosyl)-adenin und 1-(9-Adenyl)-pseudo-D-glukal werden beschrieben. Diese Substanzen wirken bei der Maus erheblich antileukämisch.     

Novel wide band gap alloyed semiconductors,x(LiGaO_2)_(1/2)-(1-x)ZnO,and fabrication of their thin films

Oxide semiconductor alloys of x(LiGaO2) 1/2-(1-x) ZnO were fabricated by the solid state reaction betweenβ-LiGaO2 and ZnO and rf-magnetron sputtering.For the solid state reaction,the wurtzite-type single phases were obtained in the composition range of x≤0.38.The formation range of the alloys was wider than that of the(Mg1-xZnx) O system,because the β-LiGaO 2possesses a wurtzite-derived structure and approximately the same lattice constants with ZnO.The electrical resistivity and energy band gap of the 0.38(LiGaO2) 1/2-0.62ZnO alloyed ceramic were 0.45-cm and 3.7 eV,respectively,at room temperature.For the alloying by sputtering,the films consisting of the wurtzite-type single phase were obtained over the entire composition range of x(LiGaO2) 1/2-(1-x) ZnO.The energy band gap was controllable in the range from 3.3 to 5.6 eV.For the as-deposited film fabricated using the 0.4(LiGaO2) 1/2-0.6ZnO alloyed ceramic target,the energy band gap was 3.74 eV,and the electrical resistivity,carrier density and the Hall mobility at room temperature were 3.6-cm,3.4×1017 cm-3and 5.6 cm 2 V-1s-1,respectively.     

Localisation of acetylcholinesterase in rat myotubes in the presence of beta-endorphin and beta-endorphin-(1-27)

In rat embryo skeletal myotubes, acetylcholinesterase is present, as multiple forms, and can be detected in deposits at the cell surface. Myotubes cultured in the presence of beta-endorphin, exhibit an increased predominance of the globular (precursor) forms of the enzyme, which are largely restricted to intracellular sites associated with nuclei. In the presence of beta-endorphin-(1-27), the relative proportions of the different forms of acetylcholinesterase is similar to that seen in the controls, but the enzyme is intracellular and has a characteristic focal localisation in the myotube.     

Antiarrhythmic properties of 3-(2-hydroxy-3 isopropylamino-propoxy)-3 phenyl-2 isoindolinone-1, (RS, SR) in the dog]

In the Dog, 3-(2-hydroxy-3 isopropylamino-proxy)-2-phenyl-1-isoindolinone (RS, SR) possesses an anti-arrhythmic activity similar to that of quinidine but at dose levels 2 to 6 times lower than in the case of the latter compound. Furthermore, in contrast to quinidine, at the dose levels where the antiarrhythmic activity is well observed, the compound is devoid of hypotensive activity and of depressive action on cardiac contractility. The first clinical studies of this compound have shown its usefulness in the treatment of ventricular and supraventricular arrhythmias.     

Effect of imazalil (1-(2-(2,4-dichlorophenyl)-2-(2-propenyloxy) ethyl)-1H-imidazole) on biosynthesis of ergosterol in Penicillium expansum Link]

Imazalil is a new fungicide effective against Penicillium molds on fruits after harvest. This compound inhibits ergosterol biosynthesis in mycelia of Penicillium expansum. The accumulation of 24--methylenedithydrolanosterol, obtusifoliol and 14 alpha-methyl-delta 8, 24(28)-ergostadienol in treated fungi suggests that imazalil blocks sterol C--14 demethylation.     

Rare electrophoretic variants of the proteins adenylate kinase 1, phosphoglucomutase 1 and 2, and transferrin (AK1, PGM1, PGM2, Tf) in two populations of French Guiana]

Two small populations of inner French Guiana were investigated for red cell enzymes and serum proteins. Rare variants were found in four systems (AK1, PGM1, PGM2, Tf). Similarities between some of these variants and those found in other Amerindian populations indicate that these genetic markers may be valuable in studies of Amerindians. A mutation rate has been estimated from the results.     

Variations in nitrogenous compounds in the urine ofStrophocheilus (pulmonata,mollusca) with different diets

Résumé La composition de l'urine du pulmoné terrestreStrophocheilus oblongus musculus, spécialement le taux de l'urée, est un reflet des différences du contenu protéique des aliments. Ce fait confirme que le fonctionnement du rein des mollusques et des vertébrés est semblable.     

The benzilic acid rearrangement of 3α,17β-Diacetoxy-11-hydroxy-12-oxo-5β-androst-9(11)-ene

Zusammenfassung Die Bildung von 11-Carboxy-3, 11, 17-trihydroxy-13-C-nor-5-androstan 11a,17-Lakton aus 3, 17-Diacetoxy-11-hydroxy-12-oxo-5-⁹(11)-androsten wird beschrieben. Der Mechanismus und die Stereochemie dieser Umwandlung (Retro-Aldolkondensation und Benzilsäureumlagerung) wird diskutiert.     

Comparison of Β-Adrenergic blocking activity of dichloroisoprenaline (H 56/28, I.C.I. 50172, LB46), methoxamine (MJ 1999) and propranolol in the canine femoral vascular bed

Zusammenfassung Die blockierende Wirkung intra- arteriell verabreichter,-adrenergischer Mittel wurde am femoralen Gefässgebiet des Hundes untersucht. DCI, H 56/28 und LB 46 per se regten den arteriellen Blutstrom mit zunehmender Dosierung an, während Methoxamin in umgekehrter Weise wirkte. Eine hemmende Wirkung auf den durch Isoprenalin angeregten Blutstrom fand sich in folgender Reihenfolge: LB 46H 56/28 > Propranolol > MJ 1999=DCI. I.C.I. 50172 und Methoxamin fehlt diese Wirkung.     

Pharmacological studies of a new analgesic,dl-erythro-1-phenyl-2-(o-chlorophenyl)-2-[4-(p-methoxybenzyl)-1-piperazinyl] ethanol dihydrochloride,in experimental animals

Summary dl-Erythro-1-phenyl-2-(o-chlorophenyl)-2-[4-(p-methoxybenzyl)-1-piperazinyl] ethanol dihydrochloride showed orally a definite analgesic activity, without producing the significant morphine-like physical dependence liability, and its analgesic potency was about a half that of codeine and far superior to aminopyrine in experimental animals.