Absorption, distribution and excretion of 1-[bis(4-fluorophenyl)methyl]-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (KB-2796) after single oral administration in rats was written by Kawashima, Tsuneo;Awata, Norio;Satomi, Osamu;Nose, Takashi;Esumi, Yoshio;Mitsugi, Koichi;Katami, Yoshiharu;Ichige, Kazumi;Hirano, Hiromi;Yatsu, Sachiko. And the article was included in Yakubutsu Dotai in 1990.Safety of 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride This article mentions the following:
The absorption, distribution and excretion of the Ca blocker KB-2796 were studied in male and female rats after single oral administration of [14C]KB-2796. The maximum blood concentration of radioactivity appeared at 1 h after administration to male rats at 2 mg/kg and the secondary peak occurred at 12 h after dosing. Thereafter the blood concentrations decreased with the terminal half-life of 42.9 h. The blood concentrations were increased proportionally to the administered doses ranging from 2 to 20 mg/kg. The blood concentrations in female rats decreased more slowly than those in male rats with a terminal half-life of 79.4 h. Male rats excreted 67.4% of the dose in bile and 6.4% in urine within 48 h after dosing; 5.7% of the dose remained in the carcass. The absorption from the intestinal tract was ∼80%. The radioactivity was mainly excreted in feces via bile and partly underwent enterohepatic circulation. The biliary excretion in female rats was lower than that in male rats and the radioactivity was slowly eliminated from the body. Tissue concentrations of radioactivity were over 3-times higher than the plasma concentrations except for the concentrations in the blood and eyeball at 6 h after administration to male rats. High levels of radioactivity were found in the lung, liver, and fat, and disappeared slowly from tissues. Tissue concentrations in female rats were higher than those in male rats. The plasma protein binding in vitro was independent of the concentration (0.04-1 μg/mL) and was about 60% in rats and 80% in humans. In vivo, 69.5-82% of radioactivity was bound to protein of male rat plasma collected 1-24 h after administration. In the experiment, the researchers used many compounds, for example, 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (cas: 101477-54-7Safety of 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride).
1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride (cas: 101477-54-7) belongs to piperazine derivatives. A form in which piperazine is commonly available industrially is as the hexahydrate, C4H10N2. 6H2O, which melts at 44 °C and boils at 125–130 °C. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. Safety of 1-(Bis(4-fluorophenyl)methyl)-4-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics