ABSTRACT
Experiments on various animals showed that fensulkal, a new phenylglyoxylic acid derivative, possesses a high antiinflammatory activity and low toxicity, markedly exceeding butadion in the therapeutic index. The mechanism of the antiphlogistic effect of fensulkal is due to its antagonism with respect to mediators of the inflammatory process and the ability of suppressing the increased permeability of capillaries and is partly related to the adrenal cortex. The drug is registered and recommended for application as antiinflammatory remedy in the form of ointment to be used for the treatment of some gynecological disorders.
Subject(s)
Acetates/therapeutic use , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Sulfonic Acids/therapeutic use , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Arthritis/chemically induced , Arthritis/drug therapy , Burns/drug therapy , Cats , Edema/chemically induced , Edema/drug therapy , Lethal Dose 50 , Mice , Pain Measurement , Peritonitis/drug therapy , Phenylbutazone/therapeutic use , Phenylbutazone/toxicity , Rabbits , Rats , Toxicity Tests, AcuteABSTRACT
Seven synthetic peptide fragments of thymic hormones were investigated using behavioral and electrophysiological methods. Splenopentin was shown to increase markedly learning capacities and memory. In contrast, alpha 1-thymosin fragment decreased them. Other peptides only slightly affected the capacities. Two active peptides seem to affect the level of activation of subcortical structures responsible for the excitation and inhibition.
Subject(s)
Hormones/pharmacology , Learning/drug effects , Memory/drug effects , Peptide Fragments/pharmacology , Thymus Hormones/pharmacology , Animals , Conditioning, Classical/drug effects , Conditioning, Classical/physiology , Dose-Response Relationship, Drug , Electroencephalography , Female , Learning/physiology , Male , Memory/physiology , Rabbits , Rats , Social BehaviorABSTRACT
The experiments on rats have shown that intraperitoneal administration of ACTH5-8 fragments in a dose of 40 ng per kg altered considerably the character of self-stimulation reaction and the behaviour of rats. Searching activity and self-stimulation reaction were intensified, with the latter characterized by the onset of aversive components, that disappeared 24 hours later. Activation depended on the site of stimulation. Two phases of activity were noted (the first 0.5-1 h and the second 4.5-6 h after ACTH5-8 injection). beta-MSH5-8 fragment, when injected intraperitoneally in a dose of 20 ng per kg, had no effect on self-stimulation reaction and the behaviour of animals.
Subject(s)
Adrenocorticotropic Hormone/physiology , Hypothalamus/physiology , Melanocyte-Stimulating Hormones/physiology , Peptide Fragments/physiology , Self Stimulation/physiology , Animals , Electric Stimulation , Hypothalamic Area, Lateral/physiology , Hypothalamus, Anterior/physiology , Male , Mammillary Bodies/physiology , Motor Activity/physiology , RatsABSTRACT
Preparative isoelectrofocusing used for fractionating the whole human granulocyte lysate serine proteinases revealed multiple forms of elastase, cathepsin G, kininogenase, human granulocytes plasminogen activator (pI 6.2-10.75). Kinetic characteristics of their substrate specificity were also obtained. It is shown that serine kininogenase of human granulocytes is not identical with elastase as it had been supposed before, it is of trypsin-like nature and is identical with plasminogen activator of these cells. The results obtained reveal new aspects in comprehension of the role of the granulocyte plasminogen activator in development of the inflammatory reaction. It is found that acid-stable proteinase inhibitors formed from blood plasma inter-alpha-inhibitor of trypsin, have an inhibitory effect on the granulocyte plasminogen activator, that supports an assumption on the anti-inflammatory function of these inhibitors.
