Psychotropic Activity of New Fluorinated Derivatives of Tetrahydrocarbasoles.

Psychotropic properties of CA-7043× and CA-7050×, new fluorinated derivatives of tetrahydrocarbasoles, were examined on outbred CD1 mice and transgenic 5×FAD mice with Alzheimer disease. Both agents exerted cognitive-stimulating and anxiolytic effects in a dose of 5 mg/kg. In the new cage test, they retarded extinction of orientation and exploratory behavior. CA-7043× produced an anxiolytic effect on CD1 mice assessed in the open-field test and exerted cognitive-stimulating action in the new location test. In the same tests, CA-7050× demonstrated the cognitive-stimulating and anxiolytic effects on transgenic 5×FAD mice.

Binary mechanism of action of cognition enhancer NT1505 on glutamate receptors.

Compound NT1505 potentiates AMPA receptors in rat brain neurons and simultaneously noncompetitively blocks NMDA receptors via two different mechanisms. Considering previously obtained data on strong cognition-enhancing properties of this compound we can conclude that NT1505 is a novel cognition stimulator exhibiting properties of a positive modulator of AMPA receptors and a blocker NMDA receptor.

[The effect of mexidol on the myelosuppressive toxicity, and on the antitumor and antimetastatic effectiveness of cyclophosphane].

Mexidol therapy inhibited cyclophosphamide-induced myelosuppression in C57B1/6 line mice with Lewis lung carcinoma without affecting antitumor action of the latter. Mexidol plus cyclophosphamide proved more effective in prophylaxis of metastasis as compared with the cytostatic alone.

[Morphogenetic aspect of the influence of purified birch tar on skin]. / Morfogeneticheskii aspekt deistviia na kozhu degtia berezovogo ochishchennogo.

Changes of the histological structure of rat's skin were studied two weeks following the daily applications of native birch tar and of purified birch tar, devoid of the components that could be potentially dangerous for humans. The morphometric investigations were performed with the use of computer technologies on the apparatus-programme complex (DiaMorph, Russia). It has been established that the main morphological manifestations of specific dermatotropic activity of birch tar in the present experiment included: epidermal hypertrophy, hyperkeratosis, stimulation of the activity of all dermal cellular elements, intensification of blood supply, reduction of sebaceous glands. Analysis of morphological findings indicates the bioequivalence of the native and purified birch tar in terms of its specific dermatotropic activity.

[Effects of interferon inducers on chemically-induced mutagenesis and carcinogenesis]. / Vliianie induktorov interferona na khimicheski indutsirovannyi mutagenez i kantserogenez.

The murine bone marrow cellular chromosomal aberration technique was used to reveal anticlastogenic effects of the natural interferon inductors ridostin and larifan, as well as the synthetic ones polyguacil and amyxin. The action of the interferon inductors was timed to the maximum production of interferon in the body. Anticarcinogenic, antitumor, and antimetastatic properties of the above interferon inductors were found by using classical experimental models of carcinogenesis. Some mechanisms of antimutagenic and coupled anticarcinogenic action of interferon inductors were considered. The natural interferon inductor larifan was found to have an antipromoter activity. The treatment regimen by using interferon inductors in combination with the immunomodulator thymosin, a thymic hormone, was under discussion.

[The testing of the carcinogenicity of dispirotripiperazine derivatives by combined administration with sodium nitrite]. / Testirovanie kantserogennosti proizvodnykh dispirotripiperaziniia pri kombinirovannom vvedenii s nitritom natriia.

The cancerogenic activity of the dispirotripiperasinium derivatives prospidine and spirobromine was tested in concurrent use with sodium nitrite. The drugs were intragastrically administered once a week. It was combined with sodium nitrite, 35 mg/kg, to non-inbred rats of both sex during 24 months. A morphological study revealed no statistically significant reduction of latency and no increase in the incidence of tumors in laboratory animals. No cancerogenic effect of sodium nitrite was found.

[The effect of experimental hepatopathy on the nature of the spontaneous metastasis of Lewis lung carcinoma]. / Vliianie éksperimental'noi gepatopatii na kharakter spontannogo metastazirovaniia kartsinomy legkikh L'iuis.

The paper deals with the effect of carbon tetrachloride-induced hepatopathy on pattern of spontaneous dissemination of Lewis tumor transplanted to C57B1/6 mice. Antitumor drugs vincristine and rubomycin prevented dissemination to the liver but failed to arrest spreading to the lung.

[The growth and metastatic characteristics of Lewis lung carcinoma during reproductive dysfunction in male C57BL/6 mice]. / Kharakteristika rosta i metastazirovaniia kartsinomy legkogo L'iuis v usloviiakh disfunktsii reproduktivnoi sistemy myshei samtsov B57BL/6.

Results of a study of the pattern of spontaneous dissemination of Lewis lung carcinoma in male mice with reproductive system dysfunction showed that removal of the gonads followed by substitution treatment with testosterone failed to influence tumor metastatic potential. The data suggested that the androgen lacked a modulating effect on growth and dissemination of Lewis lung carcinoma.

[Effects of prospidin on the development of pulmonary metastases of Lewis tumors in rats in regard to changes in the level of extracellular calcium]. / Vliianie prospidina na razvitie legochnykh metastazov opukholi L'iuis na fone izmeneniia urovnia vnekletochnogo kal'tsiia.

The effect of prospidin on Lewis lung carcinoma spreading under hyper- and hypocalcemia was studied. At early stages, increased extracellular calcium level was associated with inhibition of tumor dissemination to the lungs; however, later, colony growth was stimulated. Extracellular calcium level was shown to modulate the antitumor and antimetastatic effect of prospidin.