Pharmacokinetics and autoradiography of [3H] or [14C]stepholidine.
After iv [3H]stepholidine (SPD) 12 MBq/kg, the concentration-time curve in rats was found to be a two-compartment open model. The distribution phase T1/2 alpha = 3.6 min, the elimination phase T1/2 beta = 168 min. The absorbed radioactivities of [3H] SPD in 15-30 min were 80-87%. The amounts of [3H]SPD bound to plasma protein, liver and kidney homogenates were estimated to be 37, 31, and 30%, respectively. During 3 d after ip [3H]SPD 50 MBq/kg, 56% of the radioactivity was excreted in urine and 5% in feces, thus, it suggested that [3H]SPD was mainly excreted by kidneys. After iv a single dose of [14C]SPD in mice, the whole-body autoradiography showed that [14C]SPD was rapidly distributed among various tissues. High radioactivities were found in kidneys, liver, brain, salivary glands, Harder's glands, heart blood and muscle at 2 min and intensively localized in kidneys and stomach mucosa at 30 min. The radioactivities in these tissues disappeared 4 and 8 h later, while that in intestine could not be detected 24 h later.
Zhang
Z D
ZD
Shanghai Institute of Materia Medica, Chinese Academy of Sciences.
Zhou
C M
CM
Jin
G Z
GZ
Zhang
X
X
Yang
L
L
D000818:Animals; D001345:Autoradiography; D001599:Berberine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000652:urine; D002250:Carbon Radioisotopes; D005260:Female; D008297:Male; D051379:Mice; D051381:Rats; D011919:Rats, Inbred Strains; D014018:Tissue Distribution; D014316:Tritium
D002250:Carbon Radioisotopes; D001599:Berberine; C010513:stepholidine; D014316:Tritium