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Biomedical subjects

I Galatulas

Publications and source records attributed to I Galatulas.

At least 37 records · Page 2Linked to original sources

Potential antitumor agents X: Synthesis and antitumor activity of two nitrogen mustard derivatives related to ketocaine.

The synthesis of two nitrogen mustard derivatives (VIII and IX) related to the well-known local anesthetic ketocaine (III) is reported. These compounds were tested in mice implanted with Ehrlich ascites tumor cells, and the antitumor activity was compared with that of two previously synthesized analogues (I and II) lacking the nitro group and with that of doxorubicin. The monofunctional compound IX was inactive, but the bifunctional compound VIII showed potent antitumor activity (%T/C greater than 254 at 20 mg/kg).

Animals↗

Antinociceptive effect of centrally administered cimetidine and dimaprit in the rat.

Cimetidine, an H2 receptor antagonist, administered into a lateral ventricle of the rat brain caused a significant increase in tail flick latency. Dimaprit, a specific H2 agonist, failed to counteract the analgesic effect of cimetidine. In contrast, it enhanced the effect of cimetidine and per se had marked analgesic activity. The specific opioid antagonist naloxone was without effect. Pretreatment with CaCl2 completely prevented the action of cimetidine. These findings suggest that the analgesic action of cimetidine and dimaprit is not due to specific effects on H2 receptors.

Analgesia↗

Interaction between doxorubicin and mitomycin C on mortality and myocardial contractility in guinea pig.

The present investigations were carried out in guinea pig to ascertain whether mitomycin C has a direct cardiotoxic effect or interacts with doxorubicin-induced cardiotoxicity. I.p. administration of mitomycin C did not modify the survival rate up to 30 days, whereas the combined administration of doxorubicin and mitomycin C significantly decreased the survival time in comparison to the doxorubicin-treated group. On isolated atria, mitomycin C did not cause significant inhibition of the contractile force or an enhancement of the doxorubicin-induced negative inotropic effect. These results do not support the possibility that mitomycin C potentiates the acute cardiotoxic effects produced by doxorubicin.

Animals↗

Potential antitumor agents IX: synthesis and antitumor activity of two analogues of ketocaine.

The reaction between o-hydroxybutyrophenone and tris(2-chloroethyl)amine gave two analogues (II, V) of the well-known local anesthetic ketocaine (I). Compounds II and V showed interesting antitumor activity in mice implanted with Ehrlich ascites tumor cells (% T/C = 149 at 5 mg/kg and 171 at 50 mg/kg, respectively). Further studies on the pharmacological behavior of these new compounds are in progress.

Animals↗

Enhancement of mitogenic stimuli by phosphatidylinositol.

Phosphatidylinositol added to the medium markedly stimulated the growth-promoting effect of mitogens in normal cells (human lymphocytes and mouse embryo fibroblasts). However, it did not significantly affect quiescent cells or proliferating tumor cell lines (HeLa and MCF-7). The results are consistent with the suggested role of phosphatidylinositol in the widespread mechanism of calcium mobilization.

Adenocarcinoma↗

Reduction of lethal toxicity of doxorubicin by amrinone.

Administration of amrinone, a new inotropic agent, markedly reduced acute lethal toxicity in normal female Swiss and male BALB/c mice given lethal doses of doxorubicin. Because amrinone abolished the negative inotropic effect of doxorubicin in isolated guinea pig atria, it was suggested that partial protection from acute toxicity of the antitumor antibiotic is directly related to protection of cardiac function.

Aminopyridines↗

[Beta-lactamines].

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Anti-Bacterial Agents↗

Bactericidal and antineoplastic effect of combination of gentamicin and adriamycin.

Gentamicin and adriamycin were tested against eight strains of Proteus mirabilis: using the cellophane transfer technique, combinations of these antibiotics were screened for bactericidal activity. On mice bearing Ehrlich ascites carcinoma, the antitumoral effect of a combination of gentamicin and adriamycin was determined. Antagonism occurred with the combination in bactericidal activity and not in antitumoral activity.

Animals↗

Enhancement of propoxyphene-induced analgesia by doxepin.

The activity of the centrally acting analgesic, propoxyphene, either alone or combined with the tricyclic antidepressant, doxepin, has been studied. Doses of doxepin, in themselves lacking any analgesic effect, remarkably enhanced the analgesic activity of propoxyphene, either by the oral or intraperitoneal route. On the other hand, oral toxicity data prove that doxepin does not alter significantly propoxyphene acute toxicity.

Analgesia↗

Cardio-toxicity of Daunomycin and Adriamycin.

Our aim was to check the possibility of modifying the cardio-toxicity of Daunomycin and Adriamycin on guinea pig atria in vitro, through a reduction of calcium concentration in the medium. In a first series of tests, left and right atria still beating were put in a bath containing Tyrode solution. In order to test the influence of hypocalcic conditions on the negative inotropic effects of the two drugs. Tyrode solution contained either the usual amount of calcium or only 50% of it. In a second series of experiments isolated tissues were electrically stimulated in Krebs-bicarbonate solution. In order to avoid the spontaneous activity of the preparations, only isolated left atria were used. Again the medium contained either the normal quantity of calcium or only 50%. The reduction of calcium concentration in the medium results in a statistically significant potentiation of the negative inotropic activity of the two drugs.

Animals↗