2,4-dinitro-(pyrimidine-2-yl) thiophenol, a new drug with antimitotic properties]

A new thiopyrimidine derivative has been synthesized. It can inhibit cell multiplication in Chick embryo fibroblasts, in Mouse Ehrlich ascites tumor cells and in Rat hepatoma cells (line Rueber) cultivated in vitro.     

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.     

Origin of a mitogrenic factor for cultivated macrophages (IMF: Inflammatory Mitogenic Factor) found in exudates of non-specific acute inflammation]

The mitogenic activity of inflammatory exudate obtained from irradiated Rats is reduced. After transfer of bone marrow syngeneic cells into irradiated Rats this mitogenic activity is further decreased, while after transfer of thymic cells it is increased. It is postulated that the mitogenic activity of inflammatory exudate could be related to thymic cells and that T lymphocytes may be involved in non specific-inflammatory reactions.     

Association of brain glycoprotein (NSA 3) with neuronal membranes and with the nodes of Ranvier]

The localisation of brain glycoprotein NSA 3 was studied by means of indirect immunofluorescence on alcohol fixed, paraffin embedded sections of Rat brain. These techniques allowed the localisation of NSA 3 to the membrane of some (about 10%) of the neurons. In the white matter, the patterns were in agreement with the localisation of the Ranvier nodes. The nodes of Ranvier were also stained in peripheral nerves.     

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.     

(3H) spiroperidol binding decreases in brains of rats infected with Venezuelan equine encephalomyelitis virus1

Summary After i.p. inoculation with the Guajira strain of Venezuelan equine encephalomyelitis virus a significant decrease in the density of (³H) spiroperidol binding sites in the striatum, midbrain and frontal cortex was observed. No changes in the affinity of the receptors could be demonstrated. This finding is compatible with neuronal degeneration caused by the viral infection.Acknowledgments. This work was partially supported by Condes-Luz and Fundacite-Zulia. Butaclamol isomers were a gift of Ayerst Laboratories, Montreal, Canada.     

Effect of prostaglandin E2 (PgE2) on the biosynthesis and metabolism of noradrenaline (NA) in the isolated and perfused rabbit heart]

In isolated perfused rabbit heart, Pg E2 at concentrations ranging from 1.10(-8) to 1.10(-4) M has shown no significant action either on the biosynthesis or on the metabolism of NA. But it inhibited NA uptake, nevertheless this action was weak.     

Degradation of [3H]thymidine by a pentosyltransferase (EC 2.4.2.4) in the plasma of man and different animals

Summary [³H]Thymidine is degraded by an enzyme (thymidine phosphorylase; EC 2.4.2.4) which we have identified in the plasma of man and some animals. The presence of this enzyme in plasma or sera used to supplement culture media may, under certain experimental conditions, limit the validity of measuring the uptake of radiolabeled thymidine as a means of defining DNA synthesis.Supported in part by United States Public Health Service grant CA-17658 from the National Cancer Institute, and grant RR-05648 from the National Institutes of Health.     

Synthesis of O1.5-(beta-D-galactopyranosyl) [DMet2, Hyp5] enkephalin amide, a new highly potent analgesic enkephalin-related glycosyl peptide

A new series of O-glycosyl enkephalins has been prepared, following a convergent strategy, with high chemical yields. The galactosyl analogue, O1.5-(beta-D-galactopyranosyl) [DMet2, Hyp5] enkephalin amide proved to be one of the most potent in vivo opioid agonists synthesized up to now.     

Degradation of [3H]thymidine by a pentosyltransferase (EC 2.4.2.4) in the plasma of man and different animals.

[3H]Thymidine is degraded by an enzyme (thymidine phosphorylase; EC 2.4.2.4) which we have identified in the plasma of man and some animals. The presence of this enzyme in plasma or sera used to supplement culture media may, under certain experimental conditions, limit the validity of measuring the uptake of radiolabeled thymidine as a means of defining DNA synthesis.     

The antiviral effect of Keishi-ni-eppi-ichi-to,a tranditional Chinese herbal medicine,on influenza A2(H2N2) virus infection in mice

The antiviral effect of Keishi-ni-eppi-ichi-to (TJS-064), a traditional Chinese herbal medicine, was investigation in mice infected with influenza A₂(H₂N₂) virus. When mice exposed to 5 LD₅₀ dose of the virus were treated orally with a 70 mg/kg dose of TJS-064 1 day before and 1 day and 4 days after the infection, 100% survived over a 25-day experimental period. At the end of this period all the control mice, treated with saline alone, had died; their mean survival time in days (MSD) was 11.2 days. When mice infected with a 10 LD₅₀ dose of the virus were treated with TJS-064, the MSD was >17.4 days and there was a 50% survival rate, while the control group had a MSD of 8.7 days and 0% survival rate. No significant antiviral effect TJS-064 was observed when the agent was administered orally to mice infected with a 100 LD₅₀ or large dose of influenza virus. Pulmonary consolidation, virus titers in lung tissues and HAI titers in sera of infected mice treated with TJS-064 were all significantly lower than those of infected mice treated with saline. Interferon activities were detected in sera of mice treated with the agent at a dose of 100 mg/kg orally. Since viricidal and viristatic activities of the agent against influenza virus were not demonstrated, the antiviral effects of TJS-064 may be expressed through the host's antiviral functions including interferon production.     

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.