[The pharmacokinetic interaction of cholinolytics and cholinesterase reactivators as a reflection of the modulation of their binding in blood plasma and in brain tissue].
Radioligand assay showed that the cholinesterase (ChE) reactivators dipiroxime and benzyxime, but not carboxime, modulate selective absorption of some cholinolytics (tributam, pediphen, aprophen) in rat brain. Significant suppression of the specific binding of muscarine antagonists was recorded after chlorophos (2.LD50) intoxication. Under such conditions, the ChE reactivators induce increase in the number of binding sites and in the parameters of the constant of cholinolytic absorption on the brain membranes. It was also established by equilibrium dialysis that the binding of cholinolytics in blood plasma under the effect of ChE reactivators is reduced, leading to redistribution of their free and bound fractures, which is most favorable for tissue sorption.
Elaeva
N L
NL
Predtechenskiĭ
M B
MB
Kul'bitskiĭ
G N
GN
Babaina
E V
EV
Trefilov
V V
VV
D000818:Animals; D001921:Brain / Q000378:metabolism*; D001923:Brain Chemistry; D002250:Carbon Radioisotopes; D018680:Cholinergic Antagonists / Q000032:analysis / Q000493:pharmacokinetics* / Q000627:therapeutic use; D002801:Cholinesterase Reactivators / Q000032:analysis / Q000493:pharmacokinetics* / Q000627:therapeutic use; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D004347:Drug Interactions; D007306:Insecticides / Q000506:poisoning; D008297:Male; D010949:Plasma / Q000737:chemistry / Q000378:metabolism*; D011041:Poisoning / Q000188:drug therapy / Q000378:metabolism; D011869:Radioligand Assay; D051381:Rats; D013997:Time Factors; D014236:Trichlorfon / Q000506:poisoning; D014316:Tritium
D002250:Carbon Radioisotopes; D018680:Cholinergic Antagonists; D002801:Cholinesterase Reactivators; D007306:Insecticides; D014316:Tritium; D014236:Trichlorfon