[Physiological effects induced by dermorphin synthetic analogue--opilong].

The effects of repeated opilong injections in a dose of 50 microg/kg/day on subsequent learning of Wistar rats have been studied. The substance caused significant anxiolytic and analgesic effects, as the majority of animals could be learned (90% against 40% in control group) despite of painful stimulus preceding to education. Opilong in a small dose displaced a relation of excitatory-inhibit processes to significant prevalence of excitation although the substance was already absent in an organism for a long time. Raised peripheral sensitivity in all rats, provoked by opilong, correlated with CNS hyper excitability, expressed in stressful, neurotic psychoemotional reactions and in the form of active avoidance. The biochemical blood analysis in opilong-induced rats demonstrated the attributes of prethrombosis in the form of fibrinolysis depression and hypercoagulation. A view is expressed, that the neuromediator brain systems can be the basic point of opilong action, that are responsible for the excitatory-inhibit conditions of CNS functioning referred on maintenance of conditioned field stability.

[The effect of piyavit on hemostatic processes and fibrinolysis in patients with ischemic heart disease]. / Vliianie piiavita na protsessy gemostaza, fibrinoliza u bol'nykh ishemicheskoi bolezn'iu serdtsa.

The oral use of the drug Piavit (derived from freeze-dried medicinal leeches) in 50 patients with coronary heart disease for 7 days in a daily dose of 600 mg (20 patients) and 1200 mg (30 patients) caused a moderate dose-independent increase in enzymatic, fibrinolysis, non-enzymatic fibrinolysis and antithrombin III activity. In half the patients who had low fibrinolytic levels, the agent stimulated mainly the release of plasminogen activator on administration days of 2 and 7. In other 15 patients the activity of plasminogen activator remained unchanged, but non-enzymatic fibrinolysis enhanced. Piavit prolonged the hypocoagulative effect of heparin and aspirin in the group of patients pretreated with these drugs. There were no clinical manifestations of the disease during 7 days.

[Physico-chemical properties of the thrombolytic compound longolytin]. / Fiziko-khimicheskie svoistva tromboliticheskogo preparata longolitina.

A preparation exhibiting high fibrinolytic activity and ability to activate plasminogen was isolated from cultivation medium of Arthrobotrys longa. Homogeneous protein, obtained after gel filtration on Sephadex G-100, had molecular mass 28,600, pI-3.68-3.74, optimum activity at pH 6.0-9.0 and temperature optimum at 37 degrees. The enzyme proved to be serine proteinase as shown by analysis using inhibitors; it required thiol groups.

[Thrombolytic effect of urokinase upon various methods of administration into the body]. / Tromboliticheskoe deistvie urokinazy pri raznykh sposobakh ee vvedeniia v organizm.

A preparation of urokinase, obtained from human kidney cell culture, was administered into rats at a single dose of 5,000-10,000 U/200 g of body mass in a variety of ways using intravenous, intraperitoneal and subcutaneous inoculations. After intraperitoneal and subcutaneous administrations an increase of fibrinolytic activity in blood was more long-term although less distinct; the phase of reactive hypercoagulation was only slightly detected within 24 hrs after these procedures. Thrombin-produced provocation of thrombosis led to a lesser ratio of death in these animals as compared with the animals group administered intravenously. However, thrombolytic effect of similar doses of urokinase was the highest in intravenous administration. The fibrinolytic activity correlated well with content of the antigen (enzyme) in blood but not with the antiplasmin content in all the procedures used.

[The fibrinolysis system in recurrent myocardial infarction]. / Sistema fibrinoliza pri povtornykh infarktakh miokarda.

Studies of blood fibrinolytic activity in 112 patients with repeated acute myocardial infarction or injury to the myocardium have revealed reduced fibrinolytic activity on non-heated fibrin plates, decreased plasmin activity and euglobulin+ fraction lysis, lowered levels of plasminogen activator, total nonenzymic fibrinolysis, antithrombin III, ++FFDP, and elevated soluble complexes of fibrin-monomer level. Complications of myocardial infarction presenting as thromboembolism; ciliary arrhythmia, chronic aneurysm with thrombosis are associated with still more marked disorders of the fibrinolysis system.

[The effect of thymoptin on enzymatic fibrinolysis]. / Vliianie timoptina na protsess fermentativnogo fibrinoliza.

Stimulation of fibrinolysis, decrease in content of fibrinogen and inhibitors were observed after intravenous, intramuscular or subcutaneous administrations of thymoptine preparation (complex of peptides, isolated from mammalian thymus) at doses of 0.1 microgram, 1.0 microgram/200 g of rat body mass. A more long-term effect was found after a course of treatment involving 5 subcutaneous or intramuscular injections (1.0 microgram). Single intravenous administration of thymoptine (0.1 microgram/200 g) caused a moderate thrombolytic action. Development of thrombosis, provoked by subtotal dose of thrombin, was inhibited after subcutaneous injection of the preparation.

[Effects of tissue-type plasminogen activator from a culture of calf kidney cells on hemostasis and fibrinolysis in experimental nephritis]. / Vliianie aktivatora plazminogena tkanevo tipa iz kul'tury kletok pochki telenka na gemostaz i fibrinoliz pri éksperimental'nom nefrite.

The plasminogen activator 960 IU/mg protein activity isolated from cultured fluid of the calf kidney cells was introduced to albino rats (180-200 g) with experimental Heynmann nephritis every day during 4 days. Nephritis caused activation of haemostasis and inhibition of fibrinolysis in the blood. There was increased excretion of the fibrin, fibrinogen degradation products in urine as a results of the local fibrin deposition in diseased kidneys. The fibrinolytic activity of the cortical zone of kidney was markedly decreased. The plasminogen activator, infused to experimental animals, resulted in normalization of the altered indexes.

[Effect of the enzyme preparation longolytin on fibrinolysis in animals]. / Vliianie fermentnogo preparata longolitina na fibrinoliz u zhivotnykh.

It has been established that fibrinolytically active enzyme longolytine isolated from the culture fluid of the saprophyte fungus Arthrobotrys longa at intravenous injection favours the prolonged increase of the plasma fibrinolytic properties as well as activation of endogenic plasminogen. Maximum values of fibrinolytic activity have been marked in 5 and 30 min after enzyme intravenous injection. The plasminogen activity is high in 120 min. The fibrinolysis indexes--fibrinolytic activity of the euglobulin fraction and amount of plasminogen activator--in 3,5 and 5 times higher than in vitro at intravenous injection. The activation of coagulation system does not occur.

[Anticoagulating properties of fungal proteases tricholysine (triase) and longolytin]. / Antikoaguliantnye svoistva gribnykh proteaz trikholizina (triazy) i longolitina.

Tricholysine (triase) and longolytin, isolated from cultural fluid of two similar lower fungi Trichothecium roseum and Arthrobotrys longa, exhibited anticoagulant and fibrinolytic properties after addition to blood plasma of experimental animals. Intravenous administration of the enzymes into animals caused the following effects: an increase in fibrinolytic activity, a slight decrease of fibrinogen concentration, an inadequate elongation of recalcification time and of thrombin time. Analysis of thromboelastograms demonstrated the anticoagulant effect: index of coagulation and maximal amplitude were decreased, time of coagulation was elongated. Preparation of tricholysine exhibited low toxicity; only doses, which exceeded 80-fold the thrombolytic dose, caused death in 34% of mice after intravenous administration.

[Role of the initial level of plasminogen activator in changes in fibrinolysis]. / Rol' iskhodnogo urovnia aktivatora plazminogena v izmeneniiakh fibrinoliza v krovi.

Fibrinolytic activity of blood in rats depended on initial level of plasminogen activator. Physical exercises, tissue plasminogen activator and fungii protease (longolytin) infusions, acetylsalicylic acid and brufen significantly increased content of the plasminogen activator with low initial level and had no such effect if the initial level of plasminogen activator was high enough.

[Changes in the components of the animal fibrinolytic system induced by the action of physiological activators and enzymes of fungal origin]. / Izmeneniia komponentov fibrinoliticheskoi sistemy zhivotnykh pri deistvii fiziologicheskikh aktivartorov i fermentov gribnogo proiskhozhdeniia.

The rat fibrinolytic system components by means of intravenous injection of physiological activators (tissue plasminogen activator, urokinase) and of enzymes isolated from the Fungi imeprfecti cultures (tricholysin, longolytin) have been investigated. It has been demonstrated that the tissue plasminogen activator and urokinase exert a similar effect on fibrinolysis by inducing a short-term increase of the euglobulin fraction fibrinolytic activity but do not practically change other components of the fibrinolytic system including the antiplasmin content. Tricholysin and longolytin produce a stronger action on the fibrinolytic system by significant affecting almost all the parameters, especially the antiplasmin content. The results obtained show that physiological activators as compared with fungal enzymes possess with better thrombolytic properties.

[Plasminogen activator from a kidney cell culture]. / Aktivator plazminogena iz kul'tury kletok pochki.

Plasminogen activator (PA) isolated from kidney's cells culture (doses 10 to 5000 IE/kg) induced lysis of experimental thrombi. Lysis time decreased from 214 to 23 min after PA infusion in doses 10 to 700 IE/kg, further doses decrease from 700 to 5000IE/kg does not accelerate lysis time of thrombi. PA infusion in doses mentioned increases the activator activity of plasma and euglobulin lysis time, but does not change the fibrinolytic activity, antiplasmin content and fibrinogen concentration.

[Effect of a single administration of plasminogen tissue activator on the state of the fibrinolytic system of rat blood]. / Vliianie odnokratnogo vvedeniia tkanevogo aktivatora plazminogena na sostoianie fibrinoliticheskoi sistemy krovi krys.

Intravenous administration of tissue activator of plasminogen obtained from pig heart into the healthy rats led to increase in the fibrinolytic activity in euglobulin fraction of blood plasma and to elevation in concentration of the products of fibrin degradation /fibrinogen/. Concentration of fibrinogen, the total fibrinolytic activity, inhibitors of fibrinolysis and the length of recalcification were unaltered distinctly in the experimental conditions described.