Prozorovskii VB

References (8)

Title : [Protection of mice by carbamates cholinesterase inhibitors against poisoning by armin and its dependence on certain physico-chemical indicators] - Prozorovskii_1999_Vopr.Med.Khim_45_525
Author(s) : Prozorovskii VB , Pavlova LV , Suslova IM , Sazonova AV , Kokushkina AV
Ref : Vopr Med Khim , 45 :525 , 1999
Abstract : A series of aminostigmin derivatives with various substituents at nitrogen in the second position of the pyridine ring, has been tested. The efficacy of preventing the death of mice poisoned by armine in five of the seven substances correlates with the constant of the rate of carbamylation of acetylcholinesterase in the in vitro experiments and with the hydrophobic nature. It is suggested that the phenomenon of protection of animals against the toxic effect of organophosphorous compounds involves the "leaving portion" of the molecule of carbamates.
ESTHER : Prozorovskii_1999_Vopr.Med.Khim_45_525
PubMedSearch : Prozorovskii_1999_Vopr.Med.Khim_45_525
PubMedID: 10761219

Title : [The distant effects of acetylcholine--links in the pathogenesis of poisoning by cholinesterase inhibitors] - Skopichev_1999_Eksp.Klin.Farmakol_62_10
Author(s) : Skopichev VG , Prozorovskii VB
Ref : Eksperimentalnaia i Klinicheskaia Farmakologiia , 62 :10 , 1999
Abstract : Scanning electron microscopy showed that the capillary endothelial cells of rats poisoned by O,O-dimethyl-O(2,2-dichlorvinyl) phosphate swell and become wrinkled, while some of the cells acquire fenestrae. In 24 h. these changes become weaker. Mass deformity of erythrocytes was seen at the same time and lasted less than 24 h. Since the capillary endothelium and the erythrocytes are devoid of cholinergic innervation but possess cholinoreceptors, the occurring effects may be explained by the distant action of acetylcholine accumulating in the blood in poisoning by cholinestarase inhibitors.
ESTHER : Skopichev_1999_Eksp.Klin.Farmakol_62_10
PubMedSearch : Skopichev_1999_Eksp.Klin.Farmakol_62_10
PubMedID: 10340119

Title : [Biochemical characteristics of aminostigmine--a new anticholinesterase agent] - Prozorovskii_1996_Biokhimiia_61_690
Author(s) : Prozorovskii VB , Rozengart VI , Ardab'eva TV , Kugusheva LI , Suslova IM
Ref : Biokhimiia , 61 :690 , 1996
Abstract : The properties of aminostigmine in comparison with those of other carbamate inhibitors of cholinesterases have been studied in vitro using potentiometric titration and Ellman methods. The bimolecular constants of the inhibition rate of acetyl-, butyryl- and propionylcholinesterase were found to be equal to (8.0-14.0).10(5) (3.8-7.7).10(5) and 11.0.10(5) M-1.min-1, respectively. In terms of inhibitory activity, aminostrigmine is comparable to neostigmine methylsulphate, being inferior to physostigmine and superior to pyridistigmine. The rate of decarbamylation of acetylcholinesterase inhibited by aminostigmine measured by the dilution method, by creating excessive acetylcholine and by dialysis is characterized by k2c constants equal to (1.1-1.6).10(-2), (2.5-2.8).10(-2) and 0.025.10(-2) min-1, respectively. On the whole, aminostigmine belongs to slowly reversible inhibitors. Being carbamylated by aminostigmine, the enzyme is resistant to reactivation by TMB-4(Trimedoxime) and HI-6. At (4-6).10(-7) M aminostigmine prevents by 50% the irreversible binding of cholinesterase by certain organophosphate inhibitors of cholinesterase when the latter are used at concentrations needed to inhibit the enzymatic activity by 85-90%.
ESTHER : Prozorovskii_1996_Biokhimiia_61_690
PubMedSearch : Prozorovskii_1996_Biokhimiia_61_690
PubMedID: 8724787

Title : [The comparative clinico-experimental characteristics of aminostigmine and galanthamine used for treating poisonings by choline-blocking substances]. [Russian] - Prozorovskii_1996_Eksp.Klin.Farmakol_59_64
Author(s) : Prozorovskii VB , Velikova VD , Pshenkina NN , Vasilenko ET
Ref : Eksperimentalnaia i Klinicheskaia Farmakologiia , 59 :64 , 1996
Abstract : The results of application of cholinesterase inhibitors, aminostigmin and galantamin, for treatment of acute poisoning with cyclodol, dimedrol, and solutan of moderately grave condition are presented. Aminostigmin was shown to exhibit the more pronounced stable and universal effect. The experiments in animals showed that aminostigmine affected peripheral and central M-cholinoreactive structures and conjugated with them more actively than galantamin. Aminostigmin, but not galantamin increases the rate of dopamine circulation and content of cyclic guanozinemonophosphate in frontal brain of rats, and this effect is exhibited even under the conditions of N-cholinoreceptor blockade with amizyl.
ESTHER : Prozorovskii_1996_Eksp.Klin.Farmakol_59_64
PubMedSearch : Prozorovskii_1996_Eksp.Klin.Farmakol_59_64
PubMedID: 8704639

Title : [The toxicological characteristics of the interaction of cholinolytics with aminostigmine--a new reversible cholinesterase inhibitor]. [Russian] - Prozorovskii_1995_Eksp.Klin.Farmakol_58_57
Author(s) : Prozorovskii VB , Sazonova AV
Ref : Eksperimentalnaia i Klinicheskaia Farmakologiia , 58 :57 , 1995
Abstract : This investigation has been carried out on albino mice. In the first series of experiments, we determined the dependence of LD50 of aminostigmine on different doses of 10 cholinolytics, and conversely, the dependence of LD50 of cholinolytics on aminostigmine administration. The initial slopes of the dose-effect curves were calculated. This data form the basis for evaluation of the character and degree of interactions. We established that benactyzine, spasmolytin, ftoracizin, arpenal, atropine, ganglerone, and methacin at low doses exhibit antagonism (with decreasing activity), whereas at high doses they exhibit synergism to the toxic effect of aminostigmine. In the interaction with aminostigmine, pirenzepine and amitriptyline (M1--cholinolytics) reveal a slightly pronounced antagonism, whereas aetyrophene, a selective central N-cholinolytic, displays mutual synergism. In the second series of experiments we showed that a combination of M1-, M2-cholinolytic atropine with M1- cholinolytics does not change the efficacy of the prophylaxis of aminostigmine and physostigmine poisoning, whereas a combination with N-cholinolytic increases it.
ESTHER : Prozorovskii_1995_Eksp.Klin.Farmakol_58_57
PubMedSearch : Prozorovskii_1995_Eksp.Klin.Farmakol_58_57
PubMedID: 8704593

Title : [Aminostigmine as a cholinesterase inhibitor and as an agent for treating poisonings by cholinergic blockers]. [Russian] - Prozorovskii_1994_Eksp.Klin.Farmakol_57_13
Author(s) : Prozorovskii VB , Livanov GA , Velikova VD , Afanas'ev VV , Pavlova LV
Ref : Eksperimentalnaia i Klinicheskaia Farmakologiia , 57 :13 , 1994
Abstract : Experiments on non-inbred albino mice have demonstrated that aminostigmine is an active reversible centrally active cholinesterase inhibitor close to the properties of physostigmine, but greatly superior to it in its action duration. Clinical examinations of healthy volunteers and patients have shown that aminostigmine-induced inhibition of cholinesterase activity persists 6 hours. The agent have been found to be more highly effective in treating cholin blocker-induced intoxications than galanthamine, which manifests itself in its greater stability of the therapeutical effect achieved and in its higher ability to prevent cardiovascular events occurring in intoxication.
ESTHER : Prozorovskii_1994_Eksp.Klin.Farmakol_57_13
PubMedSearch : Prozorovskii_1994_Eksp.Klin.Farmakol_57_13
PubMedID: 7696893

Title : [Trial of cholinesterase reactivators as proserine antagonists]. [Russian] - Prozorovskii_1983_Biull.Eksp.Biol.Med_96_66
Author(s) : Prozorovskii VB , Khramova EA , Ardab'eva TV
Ref : Biulleten Eksperimentalnoi Biologii i Meditsiny , 96 :66 , 1983
Abstract : HI-6 and TMB-4(Trimedoxime) were the most effective and safe of 7 cholinesterase reactivators tested as agents for the prophylaxis of proserine poisoning of male mice. The reactivator HI-6 strongly potentiated the prophylactic efficacy of a mixture of atropine and arpenal administered in the doses sufficient for the blockade of both the m- and h-cholinoreactive systems of mice. As demonstrated by experiments in vitro, HI-6 and TMB-4(Trimedoxime) did not reacivate proserine-inhibited cholinesterase. The natural anticholinesterase activity of HI-6 was negligible. Based on the correlation of the data obtained to the reported data indicating that HI-6 has a low ganglioblocking activity it is inferred that the direct effect on the receptor is of no importance for the potentiating effect. It is assumed that HI-6 modulates the cholinoreactive systems, which leads to a dramatic increase of the efficacy of cholinolytics.
ESTHER : Prozorovskii_1983_Biull.Eksp.Biol.Med_96_66
PubMedSearch : Prozorovskii_1983_Biull.Eksp.Biol.Med_96_66
PubMedID: 6354300

Title : [Interaction of reversible inhibitors with the catalytic centers and allosteric sites of cholinesterases] - Tonkopii_1976_Biull.Eksp.Biol.Med_82_947
Author(s) : Tonkopii VD , Prozorovskii VB , Suslova IM
Ref : Biulleten Eksperimentalnoi Biologii i Meditsiny , 82 :947 , 1976
Abstract : The kinetics of inhibition of the human red blood cell cholinesterase with galanthamine tacrine and oxazyl (ambenonium) and the effect of these drugs on chick, mouse, cat and rat blood plasma enzyme activity was studied. Galanthamine proved to bind with acetylcholinesterase in the anionic areas of the catalytic centres, oxazyl interacted in the area of the allosteric anionic site, and tacrin interacted with the hydrophobic areas of the enzyme.
ESTHER : Tonkopii_1976_Biull.Eksp.Biol.Med_82_947
PubMedSearch : Tonkopii_1976_Biull.Eksp.Biol.Med_82_947
PubMedID: 1026294