ABSTRACT
According to the current understanding, the hyperactivation of platelets may lead to increased intravascular coagulation and thrombosis. Today a relevant issue is the search for new anti-thrombotic agents that are able to modulate the activity of platelet receptors, thus, influence the processes of activation and aggregation of platelets. The aim of this study was to investigate the effects of newly synthesized thiosulfonate derivatives on platelet aggregation. The activity of the compounds was tested in vitro using platelet-rich plasma. As a result of the screening test, structural formulas of four agents with high antiaggregative activity were established. These compounds inhibited ADP- and collagen-induced platelet aggregation in a dose-dependent manner. Two of these compounds were shown to be more effective inhibitors of aggregation induced by ADP (IC50 - 8-10 µM), as well as collagen (IC50 - 1.5-2.0 µM).
Subject(s)
Blood Platelets/drug effects , Platelet Aggregation Inhibitors/chemical synthesis , Platelet Aggregation/drug effects , Thiosulfonic Acids/chemical synthesis , Animals , Cells, Cultured , Dose-Response Relationship, Drug , Drug Discovery , Esters , Molecular Structure , Platelet Aggregation Inhibitors/chemistry , Platelet Aggregation Inhibitors/pharmacology , Platelet-Rich Plasma/cytology , Rabbits , Structure-Activity Relationship , Thiosulfonic Acids/chemistry , Thiosulfonic Acids/pharmacologyABSTRACT
The influence of novel biologically active substance potassium 4-toluenethiosulfonate in concentration of 4 x 10(-5) M on the changes of electrophysiological parameters of embryonic cells in early development of fish (Misgurnus fossilis L.) was investigated including the changes of membrane potential (TMP) and enzyme activity of plasmatic membranes of loach embryos during the period of synchronous division of blastomers in the early period of development. The evaluation of influence of these matters was studied and aperiodic changes of the level of TMP were shown. The diminishing of amplitude in every period by 7/12 mV and diminishing of growth of maximal values of vibrations of TMP by 39 mV in comparison to control was noticed. It was related to inhibition of some biosynthetic processes and results in the decline of activity of membrane enzyme (Na+, K(+)-ATPase) by 75.5 +/- 4.1% and 78.4 +/- 10.4% both at the action of high (4 x 10(-3) M) and low (4 x 10(-9) M) concentrations, accordingly, at first hours of development with subsequent renewal of its activity to the level of control only for the actions of low concentration.
Subject(s)
Blastomeres/enzymology , Cell Membrane/metabolism , Cypriniformes/metabolism , Embryo, Nonmammalian/enzymology , Growth Inhibitors/pharmacology , Sodium-Potassium-Exchanging ATPase/antagonists & inhibitors , Tosyl Compounds/pharmacology , Animals , Blastomeres/ultrastructure , Cypriniformes/embryology , Embryo, Nonmammalian/cytology , Embryonic Development/drug effects , Female , Growth Inhibitors/chemical synthesis , Male , Membrane Potentials/drug effects , Microscopy, Electron , Mitosis/drug effects , Sodium-Potassium-Exchanging ATPase/metabolism , Tosyl Compounds/chemical synthesisABSTRACT
Experiments on rabbits compared the X-ray, morphological, and magnetic resonance imaging of compression fractures of the vertebral body. Edema of the bone marrow of the vertebral body was ascertained to be a basic morphological substrate that evokes a modified MR signal. The data on 178 children with suspected compression fracture of the vertebral body were used to consider the potentialities of MRI and X-ray study in this pathology. The MRI semiotics of uncomplicated compression fractures of vertebral bodies is presented. The sensitivities of MRI and spondylography in the diagnosis of compression fractures of vertebral bodies were 100 and 62.5%, respectively.
Subject(s)
Echo-Planar Imaging/methods , Spinal Fractures/diagnosis , Thoracic Vertebrae/injuries , Adolescent , Animals , Child , Child, Preschool , Humans , Rabbits , Radiography , Spinal Fractures/diagnostic imaging , Spinal Fractures/pathology , Thoracic Vertebrae/diagnostic imagingABSTRACT
The influence of a new taurine derivative on hemodynamic changes induced by electrostimulation of an aortic reflexogenic zone was studied. It is shown that 3-hour electrostimulation increased total peripheral resistance and decreased cardiac output and aortic pressure. Intravenous infusion of the taurine derivative during electrostimulation normalized abnormal hemodynamic characteristics.
Subject(s)
Cardiovascular Agents/pharmacology , Hemodynamics/drug effects , Taurine/pharmacology , Animals , Aorta/physiology , Blood Pressure/drug effects , Cardiac Output/drug effects , Electric Stimulation , Electroencephalography , Heart Rate/drug effects , Rabbits , Stroke Volume/drug effects , Taurine/analogs & derivatives , Vascular Resistance/drug effectsABSTRACT
A detailed ultrasonic picture of the prostate was provided by the rectal device of Pie Medical-200 unit for 1066 patients with chronic prostatitis before and in the course of drain therapy using electrostimulator-aspirator Intraton-4. The leading ultrasonic diagnostic symptoms of chronic prostatitis are represented by various microspaces and hypoechogenic zones in different prostatic parts which reflect activity of chronic inflammatory process. The severity of the disease was determined primarily by the presence in the prostate of "true microabscesses" (microcavity of the irregular form) and pseudomicroabscesses (drop-shaped microspaces) which can be successfully drained irrespective of their number, size, location and characteristics of the content. The evidence gave grounds for design of the scheme describing pathogenesis of chronic prostatitis and its reverse dynamics in the course of drain therapy. These reverse changes closely resemble stages of ureterohydronephrosis.
Subject(s)
Electric Stimulation Therapy/instrumentation , Prostate/diagnostic imaging , Prostatitis/diagnostic imaging , Prostatitis/therapy , Adolescent , Adult , Aged , Chronic Disease , Humans , Male , Middle Aged , Monitoring, Physiologic/instrumentation , Monitoring, Physiologic/methods , Suction/instrumentation , UltrasonographyABSTRACT
On the basis of the results of clinicoroentgenological and tensographic investigations of 119 patients after traumas of the crural bones and ankle joint (2-36 yrs. ago) the authors showed the importance of roentgenofunctional investigation of the ankle joint, a patient being in a standing position with maximum flexion and extension of the foot. A specially designed footing was proposed. Of 77 patients after intra-articular fractures of the ankle bones various disorders in articular proportions, undetectable on routine roentgenography, were diagnosed in 29 by functional roentgenography. Articular changes on roentgenofunctional investigation were revealed in one patient only out of 42 patients with extra-articular fractures of the crural bones. Tensography showed disorders of foot biomechanics in all patients with subluxations in the ankle.
Subject(s)
Ankle Joint/diagnostic imaging , Tibial Fractures/physiopathology , Adult , Ankle Joint/physiopathology , Female , Follow-Up Studies , Humans , Male , Middle Aged , RadiographyABSTRACT
The influence of adenosine on hemodynamic changes induced by electrostimulation of reflexogenic zone of aorta was studied in this article. It was shown that 3-hour electrostimulation increased the total peripheral resistance and decreased cardiac output and aortic pressure. Intravenous infusion of adenosine during electrostimulation led to the normalization of main indices of hemodynamics.
