A long acting respiratory stimulating agent: 1-(4,6Bis allylamino-2-s-triazinyl)-4-(Bis p-fluorobenzhydryl) piperazine (S 2620)

Résumé La (Bis allylamino-4, 6 s-triazinyl-2)-I (bis p-fluorobenzhydryl)-4 pipérazine est un stimulant respiratoire à longue durée d'action et dépourvu d'action stimulante du système nerveux central.     

Primary liver carcinogenesis induced by the pesticide 2-(4-tert-butylphenoxy0-1-methylethyl 2-chloroethyl sulphite (Aramite)]

Wistar rats were fed, during 56 weeks, a diet containing 5 g/kg of Aramite. At the end of the treatment, all the surviving animals show, on anatomo-pathological examination, malignant proliferation of the hepatic tissue and, in certain cases, of biliary ducts. This compound, proposed in the past as acaricide in agriculture, can thus be considered as a model substance for induction of malignant liver tumors.     

Action of leucine aminopeptidase 1 and 2 (Aspergillus oryzae 410) on various synthetic peptides (author's transl)]

By use of di- or tripeptides as substrates, LAP 1 and LAP 2, 2 fractions from Aspergillus oryzae hydrolyze oligopeptides that possess leucine as N-terminal amino acid. LAP 1 fraction also hydrolyzes the histidyl bond. Both fractions have no activity towards peptides as glutathion, gly-pro-ala; they have low or no activity towards tyrosyl and tryptophanyl bond.     

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.     

The efficacy of a novel compound, (E)-1-(4′-bromo-4-biphenylyl)-1-(4-chlorophenyl)-3-dimethylaminoprop-1-ene againstTrypanosoma cruzi in mice

Summary The biological properties of a novel compound 353C with high activity againstTrypanosoma cruzi, are described. The compound was about 10 times and 20 times more effective than either benznidazole or nifurtimox respectively, in producing radical cure in mice. 353C had a long half-life and showed anti-trypanosomal properties when given to mice at weekly intervals.     

Antihypertensive agents III. Synthesis and antihypertensive activity of 3-[4-(p-fluoro-phenyl)-1,2,3,6-tetrahydro-1-pyridyl]-1-[1-(2-hydroxyethyl)-5-methyl-4-pyrazolyl]-1-propanone

Zusammenfassung 3-[4-(p-Fluorphenyl)-1,2,3,6-te-trahydro-1-pyridyl]-1-[1-(2-hydroxyaethyl)-5-methyl-4-pyrazolyl]-1-propanon (I, CIBA 4416/B-Go) senkt bei normotonischen und hypertonischen Tieren den Blutdruck. Die Drucksenkung kann hauptsächlich auf die periphere Vasodilatation sowie auf die Vasomotorenzentren bezogen werden. Ausserdem wirkt CIBA 4416/B-Go adrenolytisch.

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Previous paper:V. P. Arya, R. S. Grewal, C. L. Kaul, S. P. Ghate, D. V. Mehta andT. George, J. Pharm. Sci.58, 432 (1969).Contribution No. 243 from CIBA Research Centre.     

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.     

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

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.     

The effect of terbutaline (PINN) 1-(3.5-dihydroxyphenyl)-2-(t-butylamino)-ethanol on the choledochoduodenal sphincter

Zusammenfassung Die- Rezeptoren vom Sphinkter von Oddi werden durch Terbutalin selektiv stimuliert.