Preclinical Study of Therapeutic Efficacy of a New Russian Radiopharmaceutical 177Lu-DOTA-PSMA.

The therapeutic efficacy of a Russian radiopharmaceutical 177Lu-DOTA-PSMA was studied in vivo using male BALB/c nu/nu (nude) mice with prostate carcinoma 22Rv1 xenografts by tumor growth inhibition criterion. The mean tumor volumes in mice treated with 177Lu-DOTA-PSMA were significantly lower than in animals of the control group. There were no significant differences in the values of tumor growth inhibition between the groups of animals receiving 3.7 or 7.4 MBq of 177Lu-DOTA-PSMA.

Biodistribution of 68Ga-NODA-Aminoglucose in Intact and Tumor-Bearing Mice.

We studied the biodistribution of 68Ga-NODA-aminoglucose (68Ga-NODA-AG) in normal mice and mice with experimental model of colon adenocarcinoma tumor. It was shown that 68Ga-NODA-aminoglucose was retained in the tumor for 3 h after injection and demonstrated high level of accumulation in the tumor. Rapid clearance of radioactivity from other organs was observed. The results suggest that 68Ga-NODA-aminoglucose is a promising agent for tumor visualization by positron emission tomography.

A Comparative Study of the Pharmacokinetics of Bis- and Pentaphosphonic Acids Labeled with Gallium-68 in Rats with Experimental Model of Bone Callus.

We analyzed biodistribution of 68Ga-labeled hydroxyethylidenediphosphonic acid (68Ga-HEDP) and diethylenetriaminepentakis(methylenephosphonic acid) (68Ga-DTPMP) in Wistar rats with experimental model of bone callus. It was shown that the content of 68Ga-DTPMP and 68Ga-HEDP in bone callus was ~1.5-fold higher than in intact femur. 68Ga-DTPMP was characterized by higher stability in vivo, higher uptake in the bone tissue, and lower uptake in others visceral organs in comparison with 68Ga-HEDP. Thus, 68Ga-DTPMP had more suitable pharmacokinetic properties than 68Ga-HEDP.

Experimental Study of the Biodistribution of New Bone-Seeking Compounds Based on Phosphonic Acids and Gallium-68.

We investigate biodistribution of gallium-labeled hydroxyethylidenediphosphonic acid (68Ga-HEDP) and diethylenetriaminepentakis(methylenephosphonic acid) (68Ga-DTPMP) in intact Wistar rats. It was shown that 68Ga-DTPMP accumulated mainly in the bone tissue providing high femur/blood and femur/muscle ratios and had high stability in vivo. In contrast, 68Ga-HEDP was characterized by low stability and high uptake of radioactivity in blood throughout the study. So 68Ga-DTPMP can be considered as a new prospective radiotracer in oncology for imaging bone tissue metastasis by positron emission tomography.

[Efficiency of enterosorbents and detoxication mechanisms in immature rats with simulated hepatitis]. / Effektivnost' énterosorbentov i mekhanizmy detoksikatsii pri modelirovannom gepatite u nepolovozrelykh krys.

Different modifications of fibrous enterosorbent of the ACFM "Dnepr-MN" type exert a normalizing effect on the morphofunctional state of the liver of preadolescent rats with the model of toxic hepatitis. The distortion in the oxidation of lipids with peroxide and in the antioxidizing system protection removed, antitoxic liver function increases, which is confirmed by microsomal oxidation processes. A mediated effect of enterosorbents on the hepatocyte membrane structures is very significant for their detoxication effect.

[Diet therapy with correction of the fat component in the treatment of children with chronic cholecystocholangitis]. / Lechebnoe pitanie s korrektsiei zhirovogo komponenta v terapii detei s khronicheskimi kholetsistokholangitami.

The children suffering from chronic affections of the biliary system showed disturbances of the exocrine and esterifying function of the liver. They also had impaired concentration and disordered motor function of the gall bladder. This reverberates on the lipid spectrum of blood, bile and ion permeability of erythrocyte membranes. Comprehensive therapy in the presence of oil-enriched diet (up to 40% of the total fat amount) exerted a favourable action on the clinical course of the disease, promoted normalization of the lipid spectrum of blood and bile, and stabilization of the structural composition of the membranes. This allows recommending such a therapeutic diet as one of the components of comprehensive pathogenetically validated therapy of children with chronic cholecystocholangitis.

[Enzymatic activity of pentose cycle and the contractile function of rabbit womb as dependent on the carbon dioxide level]. / Fermentativnaia aktivnost' pentoznogo tsikla i sokratitel'naia funktsiia matkikrol'chikh pri izmenenii urovnia uglekisloty.

The in vitro experiments were carried out to study the electrical and mechanical activities of the myometrium of nonpregnant and pregnant female rabbits as well as the enzymic activity of the pentose cycle in this tissue as affected by changes in the concentration and a fixation degree of carbon dioxide. It is shown that an increase in the carbon dioxide concentration in the incubation medium decreases the enzymatic activity of nonoxidative unit of the pentose cycle, but has no effect on the carbon dioxide fixation, electrical and mechanical activity of the myometrium. The carbon dioxide fixation in the myometrium tissue during pregnancy is established to be intensified. A higher content of carbon dioxide in the medium weakens the womb with the tonic properties of prostaglandins being significantly deteriorated.

[Effect of etimizol and sodium hydroxybutyrate on the compensatory-adaptive capabilities of newborns with chronic hypoxia]. / Vliianie étimizola i oksibutirata natriia na kompensatorno-prisposobitel'nye vozmozhnosti novorozhdennykh pri khronicheskoi gipoksii.

Daily injections of 5 mg/kg of aethimizol to female rabbits during the last week of pregnancy results in normalization of the central nervous and cardiovascular systems reactions in response to a graded mechanical stimulation, in an increased ATP content in the erythrocytes, lesser acidotonic shifts in the blood and marked diminution in the number of stillbirths. Under similar conditions of the exeriment sodium oxybutyrate in a dose of 200 mg/kg did not contribute to normalization of the central nervous and cardiovascular systems response reactions, nor did it lower the acidosis in the blood and had no marked effect on the reduction in the number of stillbirths.