[The anti-ischemic effects of 3-hydroxypyridine derivatives in cerebrovascular pathology]. / Protivoishemicheskie éffekty proizvodnykh 3-oksipiridina pri tserebrovaskuliarnoi patologii.

The effect of the antioxidant mexidol and two new derivatives of 3-oxypyridine, namely LBK-10 and LBK-39 on the circulation of blood and metabolism of the brain in the postischemic period was studied in acute experiments on narcotized cats under conditions of autohemoperfusion of the cerebral vessels with a stable volume of blood. Therapeutic injection of mexidol and LBK in a dose of 20 mg/kg inhibited the development of the no-flow phenomenon and restored the ischemia damaged metabolism in the brain tissues. LBK-10 reduced the lactate content in the blood flowing from the brain and contributed to constriction of the cerebral vessels.

[The effect of 3-hydroxypyridine derivatives on postischemic disorders in the autoregulatory reactions of the cerebral vessels]. / Vliianie proizvodnykh 3-oksipiridina na postishemicheskie narusheniia autoreguliatornykh reaktsii mozgovykh sosudov.

Acute experiments on nembutal anesthetized rats showed improvement of cerebral blood flow autoregulation in the postischemic period under the effect of mexidol and the new 3-hydroxypyridine (3-HOP) derivatives LBK-10 and LBK-38 administered for prophylactic and therapeutic, purposes. The role of dopaminergic activity, solubility in lipids, and other factors in the mechanism of the activity of 3-HOP derivatives is analysed.

[The effect of mexidol on the development of experimental peroxide athero-arteriosclerosis]. / Vliianie meksidola na razvitie éksperimental'nogo perekisnogo ateroarterioskleroza.

A rabbit model of peroxide atherosclerosis was used to examine the new psychotropic drug Mexydol for its angioprotective properties. The agent was found to inhibit atheroarteriosclerotic manifestations such as hyperlipemia, activated lipid peroxidation, lower activity of the antioxidative system and to produce protective effects on the local vascular mechanisms of atherogenesis, by diminishing the severity of aortic lesion.

[A new substance with nootropic activity--N-5(hydroxynicotinoyl)-L-glutamic acid]. / Novoe veshchestvo s nootropnoi aktivnost'iu--N-5(okinikotinoil)-L-glutaminovaia kislota.

The psychopharmacological activity of a new compound--ONK-10--N-5(hydroxynicotinoyl)-L-glutamic acid was studied. It was shown in experiments on mice and rats that the compound possesses the pronounced antiamnestic and antihypoxic effects, does not disturb the conditioned reflex activity and the orientation behavior, has no anxiolytic activity and anticonvulsant properties, causes no disorder of movement coordination, is low toxic. ONK-10 is superior by its antiamnestic and antihypoxic effects to piracetam, meclophenoxat, demanol aceglumate and is not inferior to aniracetam.

[Nonspecific immunotherapy using 2,4,6-trimethylhydroxypyrimidine (OPM-111) in Mycoplasma arthritidis infection in mice]. / Nespetsificheskaia immunoterapiia 2,4,6-trimetiloksipirimidinom (OPM-111) pri infektsii myshei Mycoplasma arthritidis.

Intraperitoneal infection of mice with M. anthritidis resulted in development of necrotic lesions in the omentum, mesentery and perirenal fatty tissue. The effect of 2,4,6-trimethyloxypyrimidine on such affections was studied. It was shown that the drug had immunomodulating properties and prevented development of lesions caused by Mycoplasma.

[Relationship between the chemical structure and anticonvulsant activity of 3-hydroxypyridine derivatives]. / Zavisimost' mezhdu khimicheskim stroeniem i protivosudorozhnoi aktivnost'iu proizvodnykh 3-oksipiridina.

It was revealed in experiments on mice, that 3-hydroxypyridine derivatives possess marked anticonvulsive activity, especially in convulsions induced by GABA-ergic substances, less in corasol, maximal electroshock and strychnine induced ones. The anticonvulsive activity in the rows of 2-substituted and 2.6-disubstituted derivatives of 3-hydroxypyridine gets increased due to the introduction of larger in volume alkyl substitutes into the 2nd molecule position. Among the 2,6-disubstituted 3-hydroxypyridine derivatives, agents were revealed that are able to enhance hyperkinesis induced by 5-hydroxytryptophan.

[Antioxidants--stabilizers of the Ca2+ transport enzyme system in sarcoplasmic reticulum membranes in vivo]. / Antioksidanty--stabilizatory fermentoi sistemy transporta Ca2+ v membranakh sarkoplazmaticheskogo retikuluma in vivo.

It has been demonstrated that natural and synthetic antioxidants of different chemical structures (alpha-tocopherol, butylated hydroxytoluene, 2-ethyl-6-methyl-3-hydroxypyridine) were capable of stabilizing enzymatic Ca2+ transport in sarcoplasmic membranes of the heart and skeletal muscles in vivo. Chronic administration of water-soluble antioxidant 2-ethyl-6-methyl-3-hydroxypyridine to young and old rats resulted in the increased rate of Ca2+ transport into sarcoplasmic reticulum vesicles of the heart and skeletal muscle homogenates. Keeping rats on vitamin E-rich diets supplemented with synthetic antioxidant butylated hydroxytoluene led to stabilization of Ca2+-ATPase against thermal denaturation in sarcoplasmic reticular membranes.

[Effect of 3-hydroxypyridine derivatives on the central nervous system]. / Vliianie proizvodnykh 3-oksipiridina na tsentral'nuiu nervuiu sistemu.

Experiments on mice and rats were made to study the effect of inhibitors-antioxidants (3-hydroxypyridine derivatives) on the central nervous system. It was established that 3-hydroxypyridine derivatives (50 to 200 mg/kg) possess a broad spectrum of psychotropic effects. They cause normalization of behavior in conflict situations, exert an antiaggressive and anticonvulsant action (antagonism with corazol), are capable of potentiating the hypnotic effect of barbiturates, and of suppressing the animals' motor activity if given in high doses. Most compounds under study have antihypoxic and antiamnestic effects.