title: [Pharmacokinetics of afobazole in rats].
abstract: Afobazole pharmacokinetics was studied after the administration via different ways in rats. After oral administration, afobazole is subject to intensive biotransformation with the formation of several metabolites (M-6, M-7, and M-11). The drug and its metabolites were detected in the blood plasma for 3 h and characterized by a high elimination rate after both oral and intravenous administration. Afobazole and its main metabolite (M-11) had a medium rate of permeability into brain (the target organ): the tissue availability was 0.584 for afobazole and 0.793 for M-11. The absolute bioavailability of afobazole upon oral administration was 43.6% for. Afobazole was completely absorbed from the gastrointestinal tract of rats and characterized by the first-pass effect, after which more than 40% of administered dose entered the circulation. The parent compound was determined in extremely low amounts in urine and feces: its content in 24-h urine on the average did not exceed 0.07% of the administered dose; in 24-h feces, it did not exceed 0.05 % after intravenous administration and 0.01% after oral administration).
authors.forename: S B
authors.initials: SB
authors.lastname: Seredenin
authors.forename: A O
authors.initials: AO
authors.lastname: Viglinskaia
authors.forename: G B
authors.initials: GB
authors.lastname: Kolyvanov
authors.forename: A A
authors.initials: AA
authors.lastname: Litvin
authors.forename: O Iu
authors.initials: OIu
authors.lastname: Kravtsova
authors.forename: V P
authors.initials: VP
authors.lastname: Zherdev
mesh_terms: D000284:Administration, Oral; D000327:Adsorption; D000818:Animals; D014151:Anti-Anxiety Agents / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D001562:Benzimidazoles / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D001682:Biological Availability; D001921:Brain / Q000378:metabolism; D004333:Drug Administration Routes; D005243:Feces / Q000737:chemistry; D041981:Gastrointestinal Tract / Q000378:metabolism; D007275:Injections, Intravenous; D008297:Male; D009025:Morpholines / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D051381:Rats
chemical_list: C410924:2-((2-morpholino)ethylthio)-5-ethoxybenzimidazole; D014151:Anti-Anxiety Agents; D001562:Benzimidazoles; D009025:Morpholines