[Comparative study of the distribution of 3[H]-himantane in the brain structures and the thymus of rats].
Dynamics of distribution of 3[H]-labeled himantane (N-(adamant-2-yl) hexamethyleneimine hydrochloride), a new drug possessing antiparkinsonian and immunostimulant activity, was monitored over a time period of 10 days after single injection (10 mg/kg, i.v.) in rats. It is show that himantane exhibits a selective affinity with respect to the tissues of striatum, where up to 10(-5) M of the radioactive drug equivalent is absorbed. This is significantly greater as compared to the relative amounts of drug in the whole brain, hippocampus, cerebellum, or thymus. The accumulation of radioactive himantane in striatum increased upon oral administration, which is indicative of the formation of drug metabolites possessing higher lipophilicity.
Kovalev
G I
GI
Laboratory of Radioisotope Investigations, Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences, Baltiiskaya ul. 8, Moscow, 125315 Russia.
Rodionov
A P
AP
Petrenko
E S
ES
Zolotarev
Iu A
IuA
D000218:Adamantane / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D000818:Animals; D000978:Antiparkinson Agents / Q000493:pharmacokinetics*; D001921:Brain / Q000378:metabolism*; D002531:Cerebellum / Q000378:metabolism; D006624:Hippocampus / Q000378:metabolism; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013950:Thymus Gland / Q000378:metabolism*; D014018:Tissue Distribution
D000978:Antiparkinson Agents; C122112:N-(2-adamantyl)hexamethylenimine; D000218:Adamantane